Sitagliptin phosphateCAS# 654671-78-0 |
Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 654671-78-0 | SDF | Download SDF |
| PubChem ID | 6451150 | Appearance | Powder |
| Formula | C16H18F6N5O5P | M.Wt | 505.3 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | MK0431 phosphate | ||
| Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
| Chemical Name | (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;phosphoric acid | ||
| SMILES | C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)CC(CC3=CC(=C(C=C3F)F)F)N.OP(=O)(O)O | ||
| Standard InChIKey | IQFYVLUXQXSJJN-SBSPUUFOSA-N | ||
| Standard InChI | InChI=1S/C16H15F6N5O.H3O4P/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22;1-5(2,3)4/h4,6,9H,1-3,5,7,23H2;(H3,1,2,3,4)/t9-;/m1./s1 | ||
| 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. | ||
Sitagliptin phosphate Dilution Calculator
Sitagliptin phosphate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.979 mL | 9.8951 mL | 19.7902 mL | 39.5804 mL | 49.4756 mL |
| 5 mM | 0.3958 mL | 1.979 mL | 3.958 mL | 7.9161 mL | 9.8951 mL |
| 10 mM | 0.1979 mL | 0.9895 mL | 1.979 mL | 3.958 mL | 4.9476 mL |
| 50 mM | 0.0396 mL | 0.1979 mL | 0.3958 mL | 0.7916 mL | 0.9895 mL |
| 100 mM | 0.0198 mL | 0.099 mL | 0.1979 mL | 0.3958 mL | 0.4948 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
Sitagliptin phosphate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts
In Vitro:Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts[1]. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival[3].
In Vivo:In vivo, the ED50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats[1]. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival[4]. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs[5].
References:
[1]. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of acti
[2]. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51.
[3]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.
[4]. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9.
[5]. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32.
- Sitagliptin phosphate monohydrate
Catalog No.:BCC2111
CAS No.:654671-77-9
- Fmoc-Asn(Trt)-ol
Catalog No.:BCC2585
CAS No.:654670-89-0
- Acantrifoic acid A
Catalog No.:BCN6488
CAS No.:654663-85-1
- Phebalosin
Catalog No.:BCN4198
CAS No.:6545-99-9
- 1-Methoxyphaseollidin
Catalog No.:BCN7185
CAS No.:65428-13-9
- DL-Dab.2HCl
Catalog No.:BCC2669
CAS No.:65427-54-5
- Boc-Asn(Xan)-OH
Catalog No.:BCC3361
CAS No.:65420-40-8
- H-D-Asp-Ome
Catalog No.:BCC2896
CAS No.:65414-78-0
- Altholactone
Catalog No.:BCN4786
CAS No.:65408-91-5
- Morin hydrate
Catalog No.:BCC8214
CAS No.:654055-01-3
- Bestatin hydrochloride
Catalog No.:BCC3908
CAS No.:65391-42-6
- alpha-Isowighteone
Catalog No.:BCN4197
CAS No.:65388-03-6
- (Z)-23-Coumaroylhederagenin
Catalog No.:BCN3748
CAS No.:654678-61-2
- Naftifine HCl
Catalog No.:BCC4806
CAS No.:65473-14-5
- Esculentoside A
Catalog No.:BCN5010
CAS No.:65497-07-6
- Cyclo(Pro-Ala)
Catalog No.:BCN2427
CAS No.:65556-33-4
- Europine N-oxide
Catalog No.:BCN1977
CAS No.:65582-53-8
- 1-Hydroxyacridone
Catalog No.:BCN7524
CAS No.:65582-54-9
- 4'-Demethylepipodophyllotoxin
Catalog No.:BCN5918
CAS No.:6559-91-7
- Cerbinal
Catalog No.:BCN4199
CAS No.:65597-42-4
- Cerberic acid
Catalog No.:BCN4200
CAS No.:65597-44-6
- Ophiopogonin D'
Catalog No.:BCN2645
CAS No.:65604-80-0
- Nintedanib (BIBF 1120)
Catalog No.:BCC3661
CAS No.:656247-17-5
- Fenretinide
Catalog No.:BCC1572
CAS No.:65646-68-6
Analysis of patients with drug-induced pemphigoid using the Japanese Adverse Drug Event Report database.[Pubmed:30575097]
J Dermatol. 2019 Mar;46(3):240-244.
To clarify the incidence of drug-induced pemphigoid in Japan, we conducted a database search and analysis using the Japanese Adverse Drug Event Report database (JADER). Among the cases recorded in JADER between April 2004 and November 2017, we targeted "pemphigoid" and analyzed the patients' backgrounds, drug involvement, time of pemphigoid onset, outcomes and year reported. For cases where three or more drugs were reportedly involved, the signal index was calculated using the reporting odds ratio (ROR) method. The total number of reported pemphigoid cases was 769. Males accounted for 58% (446 cases) and patients over the age of 60 years accounted for 82% (630 cases). The most frequently reported causative drug was vildagliptin (288 cases), followed in order by Sitagliptin phosphate hydrate (102 cases), teneligliptin hydrobromide hydrate (86 cases), linagliptin (64 cases) and furosemide (46 cases). For the 27 causative drugs, the safety signal was detected by the ROR method. The median time to onset tended to be long for these drugs. For vildagliptin with the largest reported number, the value was 508 days (range, 2-1871). Analysis of outcomes demonstrated recovery or improvement in 66.3% of cases. Analysis of the years in which reports had been published revealed that the number of pemphigoid cases has increased rapidly in recent years. Our survey was able to reveal useful data on the incidence of drug-induced pemphigoid. We expect that these results will aid the early detection and treatment of this condition.
