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MedKoo Cat#: 530436 | Name: MK-4256

Description:

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

MK-4256 is a potent and selective SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes. MK-4256 demonstrated superior efficacy in a mouse oGTT model. MK-4256 reduced glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po. As compared with glipizide, MK-4256 showed a minimal hypoglycemia risk in mice.

Chemical Structure

MK-4256
MK-4256
CAS#1104599-69-0

Theoretical Analysis

MedKoo Cat#: 530436

Name: MK-4256

CAS#: 1104599-69-0

Chemical Formula: C27H23FN8O

Exact Mass: 494.1979

Molecular Weight: 494.53

Elemental Analysis: C, 65.58; H, 4.69; F, 3.84; N, 22.66; O, 3.24

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
MK4256; MK-4256; MK 4256. MDL# MFCD25976577.
IUPAC/Chemical Name
3-((1R,3R)-3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-1-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-5-methyl-1,2,4-oxadiazole
InChi Key
NTIFDLOQPKMIJK-AJTFRIOCSA-N
InChi Code
InChI=1S/C27H23FN8O/c1-15-31-26(35-37-15)27(17-12-30-36(2)14-17)24-20(19-5-3-4-6-21(19)32-24)11-22(34-27)25-29-13-23(33-25)16-7-9-18(28)10-8-16/h3-10,12-14,22,32,34H,11H2,1-2H3,(H,29,33)/t22-,27-/m1/s1
SMILES Code
CN1N=CC([C@@]2(C3=NOC(C)=N3)N[C@@H](C4=NC=C(C5=CC=C(F)C=C5)N4)CC6=C2NC7=CC=CC=C76)=C1
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
>2 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

Preparing Stock Solutions

The following data is based on the product molecular weight 494.53 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
1: He S, Dobbelaar PH, Guo L, Ye Z, Liu J, Jian T, Truong Q, Shah SK, Du W, Qi H, Bakshi RK, Hong Q, Dellureficio JD, Sherer E, Pasternak A, Feng Z, Reibarkh M, Lin M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-35. doi: 10.1016/j.bmcl.2016.02.022. PubMed PMID: 26898814. 2: Lai Z, He S, Sherer EC, Wu Z, Yu Y, Ball R, Hong Q, Yang DX, Guo L, Li D, Tuang Q, Chicchi GG, Trusca D, Tsao KL, Zhou YP, Howard AD, Nargund RP, Hagmann WK. Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3520-5. doi: 10.1016/j.bmcl.2015.06.087. PubMed PMID: 26199120. 3: He S, Lai Z, Ye Z, Dobbelaar PH, Shah SK, Truong Q, Du W, Guo L, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Reibarkh M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang B, Howard AD, Zhou YP, Nargund RP, Hagmann WK. Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53. doi: 10.1021/ml500028c. PubMed PMID: 25050159; PubMed Central PMCID: PMC4094257. 4: He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. PubMed PMID: 24900499; PubMed Central PMCID: PMC4025728.