[CAS NO. 174635-69-9] SB-222200
PRODUCTS SPECIFICATIONS [174635-69-9]
DESCRIPTION [174635-69-9]
Overview
| MDL | MFCD00944072 |
|---|---|
| Molecular Weight | 380.48 |
| Molecular Formula | C26H24N2O |
| SMILES | O=C(C1=C(C)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC |
2 Publications Citing Use of MCE
Summary
SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders [1] .
IC50 & Target
|
NK3 |
In Vitro
SB-222200 inhibits
125
I-[MePhe
7
]neurokinin B (NKB) binding to CHO cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K
i
of 4.4 nM
[1]
.
SB-222200 antagonizes NKB-induced Ca
2+
mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC
50
of 18.4 nM
[1]
.
SB-222200 is selective for hNK-3 receptors compared with hNK-1 (K
i
>100,000 nM) and hNK-2 receptors (K
i
=250 nM)
[1]
.
SB-222200 (10 nM-1 μM) produces a concentration-dependent, surmountable inhibition of NKB-induced Ca
2+
mobilization in HEK 293-hNK-3R cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SB-222200 (5 mg/kg; 30 min pretreatment) produces inhibition of behavioral responses induced by NK-3 receptor-selective agonist senktide (HY-P0187) in mice
[1]
.
SB-2222006 exhibits moderate oral bioavailability (rat 46%) and C
max
(rat 427 ng/mL) following oral administration (rat 10 mg/kg)
[1]
.
SB-2222006 exhibits terminal elimination half-life (rat 1.9 h) due to high plasma clearance (56 mL/min/kg) following intravenous administration (rat 2.5 mg/kg)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male BALB/c mice (19-21 g) [1] |
| Dosage: | 5 mg/kg |
| Administration: | Oral administration |
| Result: | Produced 57% inhibition of senktide-induced behavioral responses in mice. |
| Animal Model: | Male Sprague-Dawley rats (300-400 g) [1] |
| Dosage: | 2.5 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection and oral gavage |
| Result: | Oral bioavailability (46%), T 1/2 (1.9 h), C max (427 ng/mL). |
Appearance
Solid
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
DMSO : ≥ 100 mg/mL ( 262.83 mM )
* "≥" means soluble, but saturation unknown.
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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution
Synonyms
