MedKoo Cat#: 465484 | Name: AM10257

Description:

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

AM10257 is a CB2 antagonist. AM10257 shows a high affinity (inhibition constant [Ki]=0.08 nM for CB2), as determined by radioligand competition assays, against [3H]-CP55,940 (Kd = 0.86 nM) Importantly, the binding affinity of the crystallized CB2 construct for AM10257 is still in the sub-nanomolar range (Ki = 0.61 nM). In assays assessing the regulation of adenylyl cyclase and b-arrestin2 recruitment,AM10257 acted as an inverse agonist and competitive antagonist at CB2

Chemical Structure

AM10257
AM10257
CAS#2316841-32-2

Theoretical Analysis

MedKoo Cat#: 465484

Name: AM10257

CAS#: 2316841-32-2

Chemical Formula: C26H35N3O2

Exact Mass: 421.2729

Molecular Weight: 421.59

Elemental Analysis: C, 74.07; H, 8.37; N, 9.97; O, 7.59

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
AM10257; AM 10257; AM-10257;
IUPAC/Chemical Name
N-((3s,5s,7s)-adamantan-1-yl)-1-(5-hydroxypentyl)-4-methyl-5-phenyl-1H-pyrazole-3-carboxamide
InChi Key
FMJXYCCDMAGPLE-WXWSCJFQSA-N
InChi Code
InChI=1S/C26H35N3O2/c1-18-23(25(31)27-26-15-19-12-20(16-26)14-21(13-19)17-26)28-29(10-6-3-7-11-30)24(18)22-8-4-2-5-9-22/h2,4-5,8-9,19-21,30H,3,6-7,10-17H2,1H3,(H,27,31)/t19-,20+,21-,26?
SMILES Code
O=C(C1=NN(CCCCCO)C(C2=CC=CC=C2)=C1C)NC3(C4)C[C@@H](C[C@@H]4C5)C[C@@H]5C3
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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 421.59 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: Hu T, Zheng G, Xue D, Zhao S, Li F, Zhou F, Zhao F, Xie L, Tian C, Hua T, Zhao S, Xu Y, Zhong G, Liu ZJ, Makriyannis A, Stevens RC, Tao H. Rational Remodeling of Atypical Scaffolds for the Design of Photoswitchable Cannabinoid Receptor Tools. J Med Chem. 2021 Sep 3. doi: 10.1021/acs.jmedchem.1c01088. Epub ahead of print. PMID: 34477367. 2: Shen L, Li X, Liu J, Liu K, Liu ZJ, Hua T. Protocol for crystal structure determination of the antagonist-bound human cannabinoid receptor CB2. STAR Protoc. 2021 Jun 7;2(2):100584. doi: 10.1016/j.xpro.2021.100584. PMID: 34151302; PMCID: PMC8192724. 3: Li X, Hua T, Vemuri K, Ho JH, Wu Y, Wu L, Popov P, Benchama O, Zvonok N, Locke K, Qu L, Han GW, Iyer MR, Cinar R, Coffey NJ, Wang J, Wu M, Katritch V, Zhao S, Kunos G, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ. Crystal Structure of the Human Cannabinoid Receptor CB2. Cell. 2019 Jan 24;176(3):459-467.e13. doi: 10.1016/j.cell.2018.12.011. Epub 2019 Jan 10. PMID: 30639103; PMCID: PMC6713262.