An NK3 receptor antagonist (IC50 = 18.4 nM); selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100

SB 222200 – 10 mg

Brand:
Cayman
CAS:
174635-69-9
Storage:
-20
UN-No:
Non-Hazardous - /

SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}  

 

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SKU: 29422 - 10 mg Category:

Description

An NK3 receptor antagonist (IC50 = 18.4 nM); selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively); decreases neurokinin B-induced calcium mobilization (IC50 = 265 nM in HEK293 cells expressing the recombinant human receptor); inhibits senktide-induced contractions in isolated rabbit iris sphincter muscle at 300 nM; decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats at 500 pmol, i.c.v.; prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg)

Formal name: 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide

Synonyms: 

Molecular weight: 380.5

CAS: 174635-69-9

Purity: ≥95%

Formulation: A crystalline solid

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