LTD4 antagonist 1

Names

[ CAS No. ]:
136564-67-5

[ Name ]:
LTD4 antagonist 1

Biological Activity

[Description]:

LTD4 antagonist 1 is a potent, orally active antagonist of leukotriene D4 (LTD4) with a Ki of 0.57 nM.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor
Research Areas >> Inflammation/Immunology

[Target]

LTD4:0.57 nM (Ki)


[In Vitro]

LTD4 antagonist 1 (Compound 38b) exhibits a Ki of 0.57 nM for displacement of [3H]LTD4 on guinea pig lung membranes, a pKB of 9.93±0.14 versus LTE4 on guinea pig trachea[1].

[In Vivo]

LTD4 antagonist 1 (Compound 38b) exhibits a po ED50/iv ED50 of 1.44 and 0.036 μmol/kg in LTD4-induced bronchoconstriction in guinea pigs[1].

[References]

[1]. Robert T. Jacobs, et al. Synthesis, Structure-Activity Relationships, and Pharmacological Evaluation of a Series of Fluorinated 3-Benzyl-5-Indolecarboxamides: Identification of 4-[[5-[((2R)-2-Methyl-4,4,4-trifluorobutyl)carbamoyl]-1-methylindol-3-yl]methyl]-3methoxy-N-[(2-methylphenyl)sulfonyl]benzamide, a Potent, Orally Active Antagonist of Leukotrienes D4 and E4. Journal of Medicinal Chemistry (1994), 37(9), 1282-97.


[Related Small Molecules]

MK-571 | Zafirlukast | Pranlukast | Nedocromil | AS-35 | LY223982 | Darbufelone mesilate | LM-1484 | Quinotolast sodium | RG-12525 | RS-601 | Tipelukast | CI-949 | CP 105696 | CP-96486

Chemical & Physical Properties

[ Molecular Formula ]:
C31H32F3N3O5S

[ Molecular Weight ]:
615.66

Related Compounds