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L-655,240

Cayman Chemical Item Number 10011562

(CAS 103253-15-2)

L-655,240 (CAS 103253-15-2)

See more	Receptor Biochemistry (344) Receptor Antagonist (94) Vascular Disease (115)

Description

The lipid mediator thromboxane (TX)A₂ plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA₂ are mediated by its specific G protein-coupled receptor, referred to as the TXA₂ receptor or TP. Two isoforms, TPα and TPβ, are produced from a single gene, differ in their carboxyl termini, and form homo- and hetero-oligomers.¹ While both isoforms signal through similar pathways, they differ in the modulation by certain agonists.² L-655,240 is a potent antagonist of the TP receptor in vitro (IC₅₀ = 7 nM)^3,4 It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo.³ Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.

1 Laroche, G., Lépine, M., Thériault, C., et al. Oligomerization of the α and β isoforms of the thromboxane A₂ receptor: Relevance to receptor signaling and endocytosis. Cell Signal 17 1373-1383 (2005).

2 Wikström, K., Kavanagh, D.J., Reid, H.M., et al. Differential regulation of RhoA-mediated signaling by the TPα and TPβ isoforms of the human thromboxane A₂ receptor: Independent modulation of TPα signaling by prostacyclin and nitric oxide. Cell Signal 20(8) 1497-1512 (2008).

3 Hall, R.A., Gillard, J., Guindon, Y., et al. Pharmacology of L-655,240 (3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-indol-2-yl]2,2-dimethylpro pan oic acid); a potent, selective thromboxane/prostaglandin endoperoxide antagonist. Eur J Pharmacol 135(2) 193-201 (1987).

4 Ogletree, M.L., and Allen, G.T. Interspecies differences in thromboxane receptors: Studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. J Pharmacol Exp Ther 260 789-794 (1992).

Formal Name	1-[(4-chlorophenyl)methyl]-5-fluoro-α,α,3-trimethyl-1H-indole-2-propanoic acid
CAS Number	103253-15-2
Molecular Formula	C₂₁H₂₁ClFNO₂
Formula Weight	373.9
Formulation	A crystalline solid
Purity	≥98%
λ_max	225, 290 nm
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard ClC1=CC=C(CN2C(CC(C)(C)C(O)=O)=C(C)C3=CC(F)=CC=C32)C=C1

Background Reading

Wikström, K., Kavanagh, D.J., Reid, H.M., et al. Differential regulation of RhoA-mediated signaling by the TPα and TPβ isoforms of the human thromboxane A₂ receptor: Independent modulation of TPα signaling by prostacyclin and nitric oxide. Cell Signal 20(8) 1497-1512 (2008).

Laroche, G., Lépine, M., Thériault, C., et al. Oligomerization of the α and β isoforms of the thromboxane A₂ receptor: Relevance to receptor signaling and endocytosis. Cell Signal 17 1373-1383 (2005).

Hall, R.A., Gillard, J., Guindon, Y., et al. Pharmacology of L-655,240 (3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-indol-2-yl]2,2-dimethylpro pan oic acid); a potent, selective thromboxane/prostaglandin endoperoxide antagonist. Eur J Pharmacol 135(2) 193-201 (1987).

Ogletree, M.L., and Allen, G.T. Interspecies differences in thromboxane receptors: Studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. J Pharmacol Exp Ther 260 789-794 (1992).

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Size	Price	Quantity	Subtotal
1 mg	$48.00		$0.00
5 mg	$216.00		$0.00
10 mg	$384.00		$0.00
25 mg	$840.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-05-25. Prices are subject to change without notice.

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