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MedKoo Cat#: 574724 | Name: GPi-688

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GPi-688 is an allosteric glycogen phosphorylase inhibitor which acts at the indole site of glycogen phosphorylase. GPi-688 inhibits glucagon-mediated hyperglycemia.

Chemical Structure

GPi-688
GPi-688
CAS# 918902-32-6

Theoretical Analysis

MedKoo Cat#: 574724

Name: GPi-688

CAS#: 918902-32-6

Chemical Formula: C19H18ClN3O4S

Exact Mass: 419.0707

Molecular Weight: 419.88

Elemental Analysis: C, 54.35; H, 4.32; Cl, 8.44; N, 10.01; O, 15.24; S, 7.64

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Synonym
GPi-688, GPi 688, GPi688
IUPAC/Chemical Name
2-Chloro-N-[1-[(2R)-2,3-dihydroxypropyl]-1,2,3,4-tetrahydro-2-oxo-3-quinolinyl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
InChi Key
UICNBXVDHCBKCE-PUODRLBUSA-N
InChi Code
InChI=1S/C19H18ClN3O4S/c20-16-7-11-6-13(22-18(11)28-16)17(26)21-14-5-10-3-1-2-4-15(10)23(19(14)27)8-12(25)9-24/h1-4,6-7,12,14,22,24-25H,5,8-9H2,(H,21,26)/t12-,14?/m1/s1
SMILES Code
O=C(C1=CC(C=C(Cl)S2)=C2N1)NC3C(N(C[C@@H](O)CO)C4=C(C=CC=C4)C3)=O
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
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively.
In vitro activity:
In vitro potency of indole site inhibitors depended upon the activity state of phosphorylase a. Both inhibitors, including GPi-688 showed selectivity for liver phosphorylase a when the isoform specific activities were equal. Reference: Br J Pharmacol. 2006 Nov;149(6):775-85. https://pubmed.ncbi.nlm.nih.gov/17016495/
In vivo activity:
In the Zucker rat, glucagon resulted in an increase in blood glucose in the vehicle-treated animals (Figure 3b). GPi688 (3.75–125 μmol kg−1) also inhibited the glucagon response in the Zucker rat. Reference: Br J Pharmacol. 2007 Dec;152(8):1239-47. https://pubmed.ncbi.nlm.nih.gov/17934512/

Preparing Stock Solutions

The following data is based on the product molecular weight 419.88 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.

Recalculate based on batch purity %
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:
1. Poucher SM, Freeman S, Loxham SJ, Convey G, Bartlett JB, De Schoolmeester J, Teague J, Walker M, Turnbull AV, Charles AD, Carey F, Berg S. An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br J Pharmacol. 2007 Dec;152(8):1239-47. doi: 10.1038/sj.bjp.0707502. Epub 2007 Oct 15. PMID: 17934512; PMCID: PMC2189994. 2. Freeman S, Bartlett JB, Convey G, Hardern I, Teague JL, Loxham SJ, Allen JM, Poucher SM, Charles AD. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br J Pharmacol. 2006 Nov;149(6):775-85. doi: 10.1038/sj.bjp.0706925. Epub 2006 Oct 3. PMID: 17016495; PMCID: PMC2014651.
In vitro protocol:
1. Poucher SM, Freeman S, Loxham SJ, Convey G, Bartlett JB, De Schoolmeester J, Teague J, Walker M, Turnbull AV, Charles AD, Carey F, Berg S. An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br J Pharmacol. 2007 Dec;152(8):1239-47. doi: 10.1038/sj.bjp.0707502. Epub 2007 Oct 15. PMID: 17934512; PMCID: PMC2189994. 2. Freeman S, Bartlett JB, Convey G, Hardern I, Teague JL, Loxham SJ, Allen JM, Poucher SM, Charles AD. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br J Pharmacol. 2006 Nov;149(6):775-85. doi: 10.1038/sj.bjp.0706925. Epub 2006 Oct 3. PMID: 17016495; PMCID: PMC2014651.
In vivo protocol:
1. Poucher SM, Freeman S, Loxham SJ, Convey G, Bartlett JB, De Schoolmeester J, Teague J, Walker M, Turnbull AV, Charles AD, Carey F, Berg S. An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br J Pharmacol. 2007 Dec;152(8):1239-47. doi: 10.1038/sj.bjp.0707502. Epub 2007 Oct 15. PMID: 17934512; PMCID: PMC2189994. 2. Freeman S, Bartlett JB, Convey G, Hardern I, Teague JL, Loxham SJ, Allen JM, Poucher SM, Charles AD. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br J Pharmacol. 2006 Nov;149(6):775-85. doi: 10.1038/sj.bjp.0706925. Epub 2006 Oct 3. PMID: 17016495; PMCID: PMC2014651.
1. Freeman et al (2006) Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br.J.Pharmacol. 149 775 PMID: 17016495 2. Poucher et al (2007) An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br.J.Pharmacol. 152 1239 PMID: 17934512

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