WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H563285
CAS#: 863504-35-2
Description: GKA-71 is a potent glucokinase activator (GKA).
Hodoodo Cat#: H563285
Name: GKA-71
CAS#: 863504-35-2
Chemical Formula: C21H23N3O6S2
Exact Mass: 477.10
Molecular Weight: 477.550
Elemental Analysis: C, 52.82; H, 4.85; N, 8.80; O, 20.10; S, 13.43
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Synonym: GKA-71; GKA71; GKA 71;
IUPAC/Chemical Name: 3-[((1S)-2-Methoxy-1-methylethyl)oxy]-5-[4-(methylsulfonyl)phenoxy]-N-(3-methyl-1,2,4-thiadiazol-5-yl)benzamide
InChi Key: NXWJQVBBXSGVOG-ZDUSSCGKSA-N
InChi Code: InChI=1S/C21H23N3O6S2/c1-13(12-28-3)29-17-9-15(20(25)23-21-22-14(2)24-31-21)10-18(11-17)30-16-5-7-19(8-6-16)32(4,26)27/h5-11,13H,12H2,1-4H3,(H,22,23,24,25)/t13-/m0/s1
SMILES Code: O=C(NC1=NC(C)=NS1)C2=CC(OC3=CC=C(S(=O)(C)=O)C=C3)=CC(O[C@@H](C)COC)=C2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 477.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Baker DJ, Wilkinson GP, Atkinson AM, Jones HB, Coghlan M, Charles AD, Leighton B. Chronic glucokinase activator treatment at clinically translatable exposures gives durable glucose lowering in two animal models of type 2 diabetes. Br J Pharmacol. 2014 Apr;171(7):1642-54. PubMed PMID: 24772484; PubMed Central PMCID: PMC3966745.
2: Winzell MS, Coghlan M, Leighton B, Frangioudakis G, Smith DM, Storlien LH, Ahrén B. Chronic glucokinase activation reduces glycaemia and improves glucose tolerance in high-fat diet fed mice. Eur J Pharmacol. 2011 Aug 1;663(1-3):80-6. doi: 10.1016/j.ejphar.2011.05.009. Epub 2011 May 11. PubMed PMID: 21586282.
3: Gill D, Brocklehurst KJ, Brown HW, Smith DM. Upregulation of β-cell genes and improved function in rodent islets following chronic glucokinase activation. J Mol Endocrinol. 2011 Jul 18;47(1):59-67. doi: 10.1530/JME-10-0157. Print 2011 Aug. PubMed PMID: 21571864.