SB-408124 HydrochlorideOX1 receptor antagonist,selective and non-peptide CAS# 1431697-90-3 |
- MK-4305
Catalog No.:BCC1760
CAS No.:1030377-33-3
- Allopurinol
Catalog No.:BCC3720
CAS No.:315-30-0
- SB-674042
Catalog No.:BCC1931
CAS No.:483313-22-0
- TCS 1102
Catalog No.:BCC4063
CAS No.:916141-36-1
Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1431697-90-3 | SDF | Download SDF |
| PubChem ID | 71576692 | Appearance | Powder |
| Formula | C19H19ClF2N4O | M.Wt | 392.83 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | SB 408124 Hydrochloride;SB408124 Hydrochloride | ||
| Solubility | Soluble in DMSO | ||
| Chemical Name | 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea;hydrochloride | ||
| SMILES | CC1=NC2=C(C=C(C=C2C(=C1)NC(=O)NC3=CC=C(C=C3)N(C)C)F)F.Cl | ||
| Standard InChIKey | DIHXPSGMLOETTI-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H18F2N4O.ClH/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3;/h4-10H,1-3H3,(H2,22,23,24,26);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 | SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.
IC50 Value: 57 nM(Ki)
Target: OX1 Receptor
in vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production.
in vivo: SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). References: | |||||
SB-408124 Hydrochloride Dilution Calculator
SB-408124 Hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5456 mL | 12.7282 mL | 25.4563 mL | 50.9126 mL | 63.6408 mL |
| 5 mM | 0.5091 mL | 2.5456 mL | 5.0913 mL | 10.1825 mL | 12.7282 mL |
| 10 mM | 0.2546 mL | 1.2728 mL | 2.5456 mL | 5.0913 mL | 6.3641 mL |
| 50 mM | 0.0509 mL | 0.2546 mL | 0.5091 mL | 1.0183 mL | 1.2728 mL |
| 100 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.5091 mL | 0.6364 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. | |||||
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
SB-408124 (SB 408124) is a selective non-peptide orexin OX1 receptor antagonist .(Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). SB-408124 (SB 408124) blocks orexin-A induced grooming following oral administration in vivo.
- OTSSP167
Catalog No.:BCC4314
CAS No.:1431697-89-0
- AT7867 dihydrochloride
Catalog No.:BCC1378
CAS No.:1431697-86-7
- AT7519 trifluoroacetate
Catalog No.:BCC1377
CAS No.:1431697-85-6
- gamma-secretase modulator 3
Catalog No.:BCC1585
CAS No.:1431697-84-5
- CAL-130 Hydrochloride
Catalog No.:BCC1441
CAS No.:1431697-78-7
- CAL-130
Catalog No.:BCC1440
CAS No.:1431697-74-3
- UNC1999
Catalog No.:BCC4552
CAS No.:1431612-23-5
- H-D-Ala-OMe.HCl
Catalog No.:BCC3199
CAS No.:14316-06-4
- BMX-IN-1
Catalog No.:BCC1434
CAS No.:1431525-23-3
- GSK-LSD1 2HCl
Catalog No.:BCC5647
CAS No.:1431368-48-7
- Neotuberostemonine
Catalog No.:BCN6239
CAS No.:143120-46-1
- BQ-3020
Catalog No.:BCC5728
CAS No.:143113-45-5
- CCT241533 hydrochloride
Catalog No.:BCC1463
CAS No.:1431697-96-9
- KN-92 hydrochloride
Catalog No.:BCC1681
CAS No.:1431698-47-3
- (S)-Tedizolid
Catalog No.:BCC1294
CAS No.:1431699-67-0
- WEHI-539
Catalog No.:BCC2055
CAS No.:1431866-33-9
- K02288
Catalog No.:BCC5084
CAS No.:1431985-92-0
- 3'-O-Galloylmyricitrin
Catalog No.:BCN8268
CAS No.:143202-36-2
- WAY 267464 dihydrochloride
Catalog No.:BCC7813
CAS No.:1432043-31-6
- Nyasicol 1,2-acetonide
Catalog No.:BCN6879
CAS No.:1432057-64-1
- Catalponol methylthiomethyl ether
Catalog No.:BCC8905
CAS No.:1432057-74-3
- 10-Acetoxyscandine
Catalog No.:BCN7035
CAS No.:1432058-90-6
- 3-(3-Hydroxy-3-methylbutanyl)-2,4,6-trihydroxybenzophenone
Catalog No.:BCC8588
CAS No.:1432062-53-7
- 8-Isomulberrin hydrate
Catalog No.:BCC8789
CAS No.:1432063-35-8
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.
