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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
MK-0893 (CRA1; MK0893) is a novel, potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. MK-0893 is a reversible and competitive antagonist with high binding affinity (IC(50) of 6.6 nM) and functional cAMP activity (IC(50) of 15.7 nM). It exhibits selectivity for the glucagon receptor in comparison to other GPCRs in family B, with IC(50) values of >10000 nM for GLP-1R, VPAC1, and VPAC2, and 1020 nM for GIPR and 9200 nM for PAC1. MK-0893 inhibited the rise in glucose that glucagon caused in rhesus monkeys and hGCGR mice. In acute and chronic mouse models, it also decreased ambient glucose levels: at 3 and 10 mpk single doses, it decreased glucose (AUC 0–6 h) by 32% and 39%, respectively, in hGCGR ob/ob mice. Comparing the blood glucose levels of hGCGR mice fed a high-fat diet to those of vehicle control and lean mice, compound 9m at 3 and 10 mpk po in feed reduced blood glucose levels by 89% and 94%, respectively, by day 10. Preclinical and clinical evaluations of MK-0893 were chosen due to its advantageous biological and DMPK characteristics.
Molecular Formula |
C33H27F4N3O4
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Molecular Weight |
605.59
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Exact Mass |
605.19
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Elemental Analysis |
C, 65.45; H, 4.49; F, 12.55; N, 6.94; O, 10.57
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CAS # |
870823-19-1
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Appearance |
Solid powder
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SMILES |
C[C@@H](C1=CC=C(C=C1)C(=O)NCCC(=O)O)N2C(=CC(=N2)C3=C(C=CC(=C3)C(F)(F)F)F)C4=CC5=C(C=C4)C=C(C=C5)OC
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InChi Key |
UXPYCHMVTKGDJP-IBGZPJMESA-N
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InChi Code |
InChI=1S/C33H27F4N3O4/c1-19(20-3-5-21(6-4-20)32(43)38-14-13-31(41)42)40-30(24-8-7-23-16-26(44-2)11-9-22(23)15-24)18-29(39-40)27-17-25(33(35,36)37)10-12-28(27)34/h3-12,15-19H,13-14H2,1-2H3,(H,38,43)(H,41,42)/t19-/m0/s1
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Chemical Name |
3-[[4-[(1S)-1-[3-[2-fluoro-5-(trifluoromethyl)phenyl]-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid
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Synonyms |
MK-0893; MK 0893; MK0893; GRA-1; GRA1; GRA 1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6513 mL | 8.2564 mL | 16.5128 mL | |
5 mM | 0.3303 mL | 1.6513 mL | 3.3026 mL | |
10 mM | 0.1651 mL | 0.8256 mL | 1.6513 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00902161 | Completed | Drug: MK0893 Drug: MK0893-matched Placebo Drug: Propranolol Hydrochloride |
Type 2 Diabetes Mellitus | Merck Sharp & Dohme LLC | May 2009 | Phase 1 |
NCT02004886 | Completed | Drug: MK-0893 Drug: Metformin Drug: Placebo |
Type 2 Diabetes Mellitus | Merck Sharp & Dohme LLC | August 11, 2006 | Phase 2 |
NCT00631488 | Completed | Drug: MK-0893 Drug: Sitagliptin Drug: Metformin |
Diabetes Mellitus, Type 2 | Merck Sharp & Dohme LLC | February 2008 | Phase 2 |
NCT02012166 | Completed | Drug: MK-0893 10 mg Drug: MK-0893 40 mg Drug: MK-0893 200 mg Drug: MK-0893 1000 mg |
Type 2 Diabetes Mellitus | Merck Sharp & Dohme LLC | July 2005 | Phase 1 |