LDN193189 HydrochlorideALK inhibitor,potent and selective CAS# 1062368-62-0 |
- LDK378
Catalog No.:BCC3691
CAS No.:1032900-25-6
- AP26113
Catalog No.:BCC1069
CAS No.:1197958-12-5
- AZD-3463
Catalog No.:BCC3907
CAS No.:1356962-20-3
- SB525334
Catalog No.:BCC2531
CAS No.:356559-20-1
- TAE684 (NVP-TAE684)
Catalog No.:BCC3660
CAS No.:761439-42-3
- (R)-Crizotinib
Catalog No.:BCC1284
CAS No.:877399-52-5
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1062368-62-0 | SDF | Download SDF |
PubChem ID | 54613581 | Appearance | Powder |
Formula | C25H26Cl4N6 | M.Wt | 552.33 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | ≥16.4mg/ml in DMSO,≥23.85mg/ml in H2O | ||
Chemical Name | 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline;hydrochloride | ||
SMILES | C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3.Cl | ||
Standard InChIKey | PCCDKTWDGDFRME-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C25H22N6.ClH/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)30-13-11-26-12-14-30;/h1-10,15-17,26H,11-14H2;1H | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | LDN193189 HCl, the hydrochloride salt of LDN193189, is a selective inhibitor of BMP signaling with IC50 of 5 nM and 30 nM for the transcriptional activity of the BMP type I receptors ALK2 and ALK3 , respectively.|ALK3 | |||||
Targets | 5 nM | 30 nM |
LDN193189 Hydrochloride Dilution Calculator
LDN193189 Hydrochloride Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.8105 mL | 9.0526 mL | 18.1051 mL | 36.2102 mL | 45.2628 mL |
5 mM | 0.3621 mL | 1.8105 mL | 3.621 mL | 7.242 mL | 9.0526 mL |
10 mM | 0.1811 mL | 0.9053 mL | 1.8105 mL | 3.621 mL | 4.5263 mL |
50 mM | 0.0362 mL | 0.1811 mL | 0.3621 mL | 0.7242 mL | 0.9053 mL |
100 mM | 0.0181 mL | 0.0905 mL | 0.1811 mL | 0.3621 mL | 0.4526 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Abstract
LDN-193189 affects all known BMP-induced signaling cascades, where it affects both Smad and non-Smad signaling pathways and inhibits activation of p38, ERK1/2 and Akt in C2C12 cells.
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
LDN193189 is a selective transcriptional activity morphogenetic protein (BMP) type I receptors inhibitor. It inhibits activin receptor-like kinase-2 (ALK2) and ALK3 with IC50 values of 5 nM and 30 nM, respectively [1].
LDN193189 has been showed to inhibit BMP induced phosphorylation of Smad signaling (Smad1/5/8) and non-Smad signaling including p38 and Akt in C2C12 cells [2].
Pharmacological inhibition of BMP by LDN193189 has shown to prevent down-regulation of E-cadherin in response to BMP2 both in bronchial epithelial (Beas2B) cells and in C57BL/6 mice. LDN193189 also inhibits the BMP-induced reduction of epithelial permeability at cellular level [3].
References:
[1] Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW, McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y, Peterson RT, Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9.
[2] Boergermann JH1, Kopf J, Yu PB, Knaus P. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol. 2010 Nov;42(11):1802-7.
[3] Helbing T1, Herold EM, Hornstein A, Wintrich S, Heinke J, Grundmann S, Patterson C, Bode C, Moser M. Inhibition of BMP activity protects epithelial barrier function in lung injury. J Pathol. 2013 Sep;231(1):105-16. doi: 10.1002/path.4215. Epub 2013 Jul 10.
- ML347
Catalog No.:BCC5331
CAS No.:1062368-49-3
- LDN-193189
Catalog No.:BCC3687
CAS No.:1062368-24-4
- Ro3280
Catalog No.:BCC3962
CAS No.:1062243-51-9
- WYE-354
Catalog No.:BCC1059
CAS No.:1062169-56-5
- WYE-687
Catalog No.:BCC4604
CAS No.:1062161-90-3
- WAY-600
Catalog No.:BCC4607
CAS No.:1062159-35-6
- TC-G 1004
Catalog No.:BCC6165
CAS No.:1061747-72-5
- PND-1186
Catalog No.:BCC1866
CAS No.:1061353-68-1
- Senktide
Catalog No.:BCC6921
CAS No.:106128-89-6
- Hoechst 33342 analog 2
Catalog No.:BCC1631
CAS No.:106050-84-4
- Palmatine hydrochloride
Catalog No.:BCN5914
CAS No.:10605-02-4
- β-Interleukin I (163-171), human
Catalog No.:BCC1017
CAS No.:106021-96-9
- Thioperamide
Catalog No.:BCC6734
CAS No.:106243-16-7
- 4-[(4-Methylpiperazin-1-yl) methyl]benzoic acid dihydrochloride
Catalog No.:BCC8669
CAS No.:106261-49-8
- Risperidone
Catalog No.:BCC3850
CAS No.:106266-06-2
- Sikokianin A
Catalog No.:BCN3133
CAS No.:106293-99-6
- Nomilin
Catalog No.:BCN1034
CAS No.:1063-77-0
- Rufinamide
Catalog No.:BCC5078
CAS No.:106308-44-5
- DAPTA
Catalog No.:BCC5909
CAS No.:106362-34-9
- ω-Conotoxin GVIA
Catalog No.:BCC5700
CAS No.:106375-28-4
- Boc-D-Alaninol
Catalog No.:BCC2727
CAS No.:106391-86-0
- Boc-D-Valinol
Catalog No.:BCC2692
CAS No.:106391-87-1
- Deoxymorellin
Catalog No.:BCN3067
CAS No.:1064-34-2
- Acid Black 1
Catalog No.:BCC8806
CAS No.:1064-48-8
Compatibility and Stability of Rolapitant Injectable Emulsion Admixed with Intravenous Palonosetron Hydrochloride.[Pubmed:28346200]
Int J Pharm Compd. 2017 Jan-Feb;21(1):76-82.
Neurokinin-1 receptor antagonist, 5-hydroxytryptamine-3 RA, and dexamethasone combination therapy is standard of care for the prevention of chemotherapy-induced nausea and vomiting. Herein we describe the physical and chemical stability of rolapitant injectable emulsion 166.5 mg in 92.5 mL (185 mg hydrochloride salt) admixed with palonosetron injection 0.25 mg in 5 mL (0.28 mg hydrochloride salt). Admixtures were prepared and stored in two types of container closures (110-mL Crystal Zenith plastic and glass bottles) and four types of intravenous administration sets (or intravenous tubing sets). Assessment of the physical and chemical stability was conducted on the admixtures in the ready-to-use container closure systems as supplied by the manufacturer, stored at room temperature (20 degrees C to 25 degrees C under fluorescent light), and evaluated at 0, 1, and 6 hours; 1 and 2 days; and under refrigeration (2 degrees C to 8 degrees C protected from light) after 1, 3, and 7 days. For admixtures in intravenous tubing sets, the assessment of physicochemical stability was performed after 0 and 7 hours of storage at 20 degrees C to 25 degrees C initially, and then after 20 hours (total 27 hours) at 2 degrees C to 8 degrees C protected from light. Physical stability was assessed by visual examination of the container contents under normal room light, and measuring turbidity and particulate matter. Chemical stability was assessed by measuring the pH of the admixture and determining drug concentrations and impurity levels with high-performance liquid chromatographic analysis. The results indicated that all samples were physically compatible throughout the duration of the study. The pH, turbidity, and particulate matter of the admixture stayed within narrow and acceptable ranges. Rolapitant admixed with palonosetron was chemically stable when admixed in glass and Crystal Zenith bottles for at least 48 hours at room temperature and for 7 days under refrigeration, as well as in the four selected intravenous tubing sets for 7 hours at 20 degrees C to 25 degrees C and then for 20 hours at 2 degrees C to 8 degrees C. No loss of potency of any admixed components occurred in the samples stored at the two temperature ranges and time period studied.
[The Discovery, Research and Development of Etelcalcetide Hydrochloride, the World 1st Intravenous Calcimimetics.][Pubmed:28336830]
Clin Calcium. 2017;27(4):537-545.
Etelcalcetide hydrochloride is the first intravenous calcimimetics agent for secondary hyperparathyroidism (SHPT). Etelcalcetide hydrochloride is to be administered through dialysis circuit by physician or medical staff upon completion of dialysis and such administration is expected to reduce the burden of medication in patients. From the nonclinical study results, etelcalcetide functions as an allosteric activator of calcium-sensing receptor(CaSR). Etelcalcetide suppressed PTH secretion both in vitro and in vivo. In a rat model of chronic renal insufficiency, etelcalcetide suppressed SHPT disorders, such as parathyroid gland hypertrophy, bone disorder, and ectopic calcification. In conclusion, etelcalcetide hydrochloride is expected to exhibit therapeutic effect against each SHPT condition by decreasing blood PTH concentrations via CaSR-agonist activity in the clinical situation.
Study on the interaction of 6-(2-morpholin-4-yl-ethyl)-6H-indolo [2,3-b]quinoxaline hydrochloride with human serum albumin by fluorescence spectroscopy.[Pubmed:28355158]
Methods Appl Fluoresc. 2016 Sep 14;4(3):034012.
Under physiological conditions, in vitro interaction between the bio-active substance 6-(2-morpholin-4-yl-ethyl)-6H-indolo[2,3-b]quinoxaline hydrochloride (MIQ) and human serum albumin (HSA) was investigated at an excitation wavelength 260 nm and at different temperatures (298 K, 308 K and 313 K) by fluorescence emission spectroscopy. From spectral analysis, MIQ showed a strong ability to quench the intrinsic fluorescence of HSA through a static quenching procedure. The binding constant is estimated asK A = 2.55 x 10(-4) l . mol(-1) at 298 K. Based on the thermodynamic parameters evaluated from the van 't Hoff equation, the enthalpy change (DeltaH degrees ) and entropy change (DeltaS degrees ) were derived to be negative values. A value of 2.37 nm for the average distance r between MIQ (acceptor) and tryptophan residues of HSA (donor) was derived from the fluorescence resonance energy transfer. UV/vis absorption spectra were used to confirm the quenching mechanism.
Identification of pyrolysis products of the new psychoactive substance 2-amino-1-(4-bromo-2,5-dimethoxyphenyl)ethanone hydrochloride (bk-2C-B) and its iodo analogue bk-2C-I.[Pubmed:28371351]
Drug Test Anal. 2018 Jan;10(1):229-236.
2-Amino-1-(4-bromo-2,5-dimethoxyphenyl)ethanone hydrochloride (bk-2C-B) has recently emerged as a new psychoactive substance (NPS). It is most commonly consumed orally, although there are indications that it might also be ingested by inhalation or 'smoking'. Information about the stability of bk-2C-B when exposed to heat is unavailable and the potential for pyrolytic degradation and formation of unknown substances available for inhalation prompted an investigation using a simulated 'meth pipe' scenario. Twelve products following pyrolysis of bk-2C-B were detected and verified by organic synthesis of the corresponding standards. In addition, 2-amino-1-(4-iodo-2,5-dimethoxyphenyl)ethanone hydrochloride (bk-2C-I) was characterized for the first time and subjected to pyrolysis as well. Similar products were formed, which indicated that the replacement of the bromo with the iodo substituent did not affect the pyrolysis pattern under the conditions used. Two additional products were detected in the bk-2C-I pyrolates, namely 1-(2,5-dimethoxyphenyl)-ethanone and 1-iodo-4-ethenyl-5-methoxyphenol. The potential ingestion of pyrolysis products with unknown toxicity adds an element of concern. Copyright (c) 2017 John Wiley & Sons, Ltd.