TM 38837 - ≥98%(HPLC), high purity , CAS No.1253641-65-4, Antagonist of CB 1 receptor;Antagonist of CB 2 receptor

Item Number

T287414

Grouped product items
SKU	Size	Availability	Price
T287414-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$162.90
T287414-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$216.90
T287414-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$488.90
T287414-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$597.90
T287414-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,033.90

Highly potent CB1inverse agonist; peripherally restricted

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Basic Description

Synonyms	Q7670627 \| 1-(2,4-dichlorophenyl)-4-ethyl-N-piperidin-1-yl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]thiophen-2-yl]pyrazole-3-carboxamide \| CS-0045262 \| HY-112340 \| 1253641-65-4 \| DTXSID301018782 \| VQOCBFYUDSBDCZ-UHFFFAOYSA-N \| AMY9051 \| EX-A6357 \| BCP24
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Highly potent cannabinoid 1 receptor (CB1) inverse agonist (IC50values are 8.5 nM and 605 nM for inhibition of [3H]-CP 55940 binding at CB1and CB2receptors, respectively). Displays 71-fold selectivity for CB1receptors over CB2receptors. Inhibits GTP bindi
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Antagonist of CB 1 receptor;Antagonist of CB 2 receptor

Associated Targets(Human)

CNR1 Tclin Cannabinoid receptor 1 (3 Activities)

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNR2 Tchem Cannabinoid receptor 2 (1 Activities)

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Names and Identifiers

IUPAC Name	1-(2,4-dichlorophenyl)-4-ethyl-N-piperidin-1-yl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]thiophen-2-yl]pyrazole-3-carboxamide
INCHI	InChI=1S/C30H25Cl2F3N4OS/c1-2-23-27(29(40)37-38-16-4-3-5-17-38)36-39(25-14-11-21(31)18-24(25)32)28(23)26-15-13-22(41-26)12-8-19-6-9-20(10-7-19)30(33,34)35/h6-7,9-11,13-15,18H,2-5,16-17H2,1H3,(H,37,40)
InChi Key	VQOCBFYUDSBDCZ-UHFFFAOYSA-N
Canonical SMILES	CCC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(S4)C#CC5=CC=C(C=C5)C(F)(F)F
Isomeric SMILES	CCC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(S4)C#CC5=CC=C(C=C5)C(F)(F)F
Alternate CAS	1253641-65-4
PubChem CID	49779607
MeSH Entry Terms	TM38837
Molecular Weight	617.51

References

1. Hung MS, Chang CP, Li TC, Yeh TK, Song JS, Lin Y, Wu CH, Kuo PC, Amancha PK, Wong YC et al.. (2010) Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist.. ChemMedChem, 5 (9): (1439-43). [PMID:20652930] [10.1021/op500134e]

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Basic Description