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GRA Ex-25
CAS No. 307983-31-9
GRA Ex-25( GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25 )
Catalog No. M13984 CAS No. 307983-31-9
A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 73 | In Stock |
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| 5MG | 128 | In Stock |
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| 10MG | 194 | In Stock |
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| 25MG | 397 | In Stock |
|
| 50MG | 584 | In Stock |
|
| 100MG | 833 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGRA Ex-25
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NoteResearch use only, not for human use.
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Brief DescriptionA potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors.
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DescriptionA potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors; binds to human glucagon receptor with Ki of 63 nM, moderately inhibits glucagon induced adenylate cyclase (Ki=254 nM); significantly reduces blood glucose caused by exogenous administration of glucagon in rat model (3 mg/kg, i.v.).Diabetes Preclinical.
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In VitroGRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively).
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In VivoGRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output.
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SynonymsGRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25
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PathwayGPCR/G Protein
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TargetGlucagon Receptor
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Recptorhumanglucagonreceptor|ratglucagonreceptor
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Research AreaMetabolic Disease
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IndicationDiabetes
Chemical Information
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CAS Number307983-31-9
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Formula Weight563.6085
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Molecular FormulaC29H36F3N3O5
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 32 mg/mL
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SMILESC[C@](C1CC[C@H](N(C(NC2C=CC(OC(F)(F)F)=CC=2)=O)CC2C=CC(C(NCCC(O)=O)=O)=CC=2)CC1)(C)C
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Chemical Nameβ-Alanine, N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Kurukulasuriya R, et al. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50.
2. Lau J, et al. J Med Chem. 2007 Jan 11;50(1):113-28.
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