Product Details
| Product Name:
SB-222200 |
CAS No.:
174635-69-9 |
| Purity:
97.13% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | SB-222200 |
| Description | SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (262.83 mM)
|
| Keywords | NKB | NK-3R | NK receptor | SB222200 | penetrant | inhibit | CNS | Neurokinin Receptor | Tachykinin receptor | nervous | central | SB-222200 | system | Inhibitor | SB 222200 | neurokinin-B | disorders |
| Inhibitors Related | Lanepitant 2HCl | Rolapitant | Ezlopitant | (R)-CJ 11974 | N-Acetyl-L-tryptophan | Netupitant | Aprepitant | Vofopitant dihydrochloride | Befetupitant | Vofopitant | Fosaprepitant dimeglumine | Maropitant |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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