AM-5262

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

MedKoo CAT#: 530482

CAS#: 1222088-90-5

Description: AM-5262 is a Potent GPR40 Full Agonist with improved rat PK profile and general selectivity profile. AM-5262 enhanced glucose stimulated insulin secretion (mouse and human islets) and improved glucose homeostasis in vivo (OGTT in HF/STZ mice) when compared to AM-1638. GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to its unique mechanism leading to little risk of hypoglycemia.

Chemical Structure

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AM-5262
CAS# 1222088-90-5
Instruction

Theoretical Analysis

MedKoo Cat#: 530482
Name: AM-5262
CAS#: 1222088-90-5
Chemical Formula: C33H35FO4
Exact Mass: 514.25
Molecular Weight: 514.637
Elemental Analysis: C, 77.02; H, 6.86; F, 3.69; O, 12.44

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: AM-5262; AM 5262; AM5262.

IUPAC/Chemical Name: (1R,2R)-6'-((2-((R)-2,2-dimethylcyclopentyl)-2'-fluoro-5'-methoxy-[1,1'-biphenyl]-4-yl)methoxy)-2',3'-dihydrospiro[cyclopropane-1,1'-indene]-2-carboxylic acid

InChi Key: XPLWBHWPOUEOSJ-RSKOUFDESA-N

InChi Code: InChI=1S/C33H35FO4/c1-32(2)13-4-5-27(32)25-15-20(6-10-24(25)26-16-22(37-3)9-11-30(26)34)19-38-23-8-7-21-12-14-33(28(21)17-23)18-29(33)31(35)36/h6-11,15-17,27,29H,4-5,12-14,18-19H2,1-3H3,(H,35,36)/t27-,29?,33-/m0/s1

SMILES Code: CC1(C)CCC[C@H]1C2=C(C3=C(F)C=CC(OC)=C3)C=CC(COC4=CC=C(CC[C@@]56[C@]([H])(C(O)=O)C6)C5=C4)=C2

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 514.64 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:
In vitro protocol:
In vivo protocol:

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1: Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown
SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran
T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL,
Chow D, Wong S, Luo J, Lin DC, Medina JC. Discovery and Optimization of Potent
GPR40 Full Agonists Containing Tricyclic Spirocycles. ACS Med Chem Lett. 2013 May
7;4(6):551-5. doi: 10.1021/ml300427u. PubMed PMID: 24900707; PubMed Central
PMCID: PMC4027505.


2: Hauge M, Vestmar MA, Husted AS, Ekberg JP, Wright MJ, Di Salvo J, Weinglass
AB, Engelstoft MS, Madsen AN, Lückmann M, Miller MW, Trujillo ME, Frimurer TM,
Holst B, Howard AD, Schwartz TW. GPR40 (FFAR1) - Combined Gs and Gq signaling
in vitro is associated with robust incretin secretagogue action ex vivo and
in vivo. Mol Metab. 2014 Oct 24;4(1):3-14. doi: 10.1016/j.molmet.2014.10.002.
PubMed PMID: 25685685; PubMed Central PMCID: PMC4314522.


3: Christensen LW, Kuhre RE, Janus C, Svendsen B, Holst JJ. Vascular, but not
luminal, activation of FFAR1 (GPR40) stimulates GLP-1 secretion from isolated
perfused rat small intestine. Physiol Rep. 2015 Sep;3(9). pii: e12551. doi:
10.14814/phy2.12551. PubMed PMID: 26381015; PubMed Central PMCID: PMC4600392.