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SB-222200

Catalog No. T16849 CAS 174635-69-9

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

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SB-222200, CAS 174635-69-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 103.00
25 mg	In stock	$ 253.00
50 mg	In stock	$ 485.00
100 mg	In stock	$ 693.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.97%

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Description	SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).
Targets&IC50	NK3:Ki=4.4 nM
In vitro	SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) [1].
In vivo	In mice, oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5 mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with the brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% [1].

Molecular Weight	380.48
Formula	C26H24N2O
CAS No.	174635-69-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (262.83 mM)

References and Literature

1. Sarau HM, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Bioactive Compound Library Neuronal Signaling Compound Library Orally Active Compound Library NO PAINS Compound Library Bioactive Compounds Library Max CNS-Penetrant Compound Library

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Keywords

SB-222200 174635-69-9 GPCR/G Protein Neuroscience Neurokinin receptor NKB NK-3R NK receptor SB222200 penetrant inhibit CNS Neurokinin Receptor Tachykinin receptor nervous central system Inhibitor SB 222200 neurokinin-B disorders inhibitor

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