1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. SB-222200

SB-222200 

Cat. No.: HY-15722 Purity: 99.85%
Handling Instructions

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

For research use only. We do not sell to patients.

SB-222200 Chemical Structure

SB-222200 Chemical Structure

CAS No. : 174635-69-9

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10 mM * 1 mL in DMSO USD 172 In-stock
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Description

SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier. IC50 Value: 4.4 nM ( Ki for hNK-3 receptor); 250 nM( Ki for hNK-2 receptor) [1] Target: NK3 Receptor 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 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

SMILES

O=C(C1=C(C)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[[email protected]](C4=CC=CC=C4)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (262.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6283 mL 13.1413 mL 26.2826 mL
5 mM 0.5257 mL 2.6283 mL 5.2565 mL
10 mM 0.2628 mL 1.3141 mL 2.6283 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.85%

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Keywords:

SB-222200SB222200SB 222200Neurokinin ReceptorNK receptorInhibitorinhibitorinhibit

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Product name:
SB-222200
Cat. No.:
HY-15722
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