SB-222200
Based on 6 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.85%
- CAS. Nr.: 174635-69-9
- Formel: C26H24N2O
- Molecular Weight:380.48
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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GPCR/G Protein Compound Library
HY-L006
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Publications Citing Use of MedChemExpress (MCE) SB-222200
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Biologische Aktivität
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NK3R |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
6.7 nM
Compound: SB 222200
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Displacement of [3H]SR142801 from human recombinant NK3 receptor expressed in CHO cells
Displacement of [3H]SR142801 from human recombinant NK3 receptor expressed in CHO cells
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[PMID: 26988801] |
| CHO | IC50 |
6.7 nM
Compound: SB 222200
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Displacement of [3H]SR142801 from human recombinant NK3 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]SR142801 from human recombinant NK3 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
| CHO | IC50 |
6.7 x 10-9 M
Compound: SB 222200
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Displacement of [3H]SR142801 from human recombinant NK3 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]SR142801 from human recombinant NK3 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
SB-222200 inhibits 125I-[MePhe7]neurokinin B (NKB) binding to CHO cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a Ki of 4.4 nM[1].
SB-222200 antagonizes NKB-induced Ca2+ mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC50 of 18.4 nM[1].
SB-222200 is selective for hNK-3 receptors compared with hNK-1 (Ki>100,000 nM) and hNK-2 receptors (Ki=250 nM)[1].
SB-222200 (10 nM-1 μM) produces a concentration-dependent, surmountable inhibition of NKB-induced Ca2+ mobilization in HEK 293-hNK-3R cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SB-2222006 exhibits moderate oral bioavailability (rat 46%) and Cmax (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (19-21 g)[1]
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Dosage:5 mg/kg
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Administration:Oral administration
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Result:Produced 57% inhibition of senktide-induced behavioral responses in mice.
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Animal Model:Male Sprague-Dawley rats (300-400 g)[1]
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Dosage:2.5 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:Intravenous injection and oral gavage
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Result:Oral bioavailability (46%), T1/2 (1.9 h), Cmax (427 ng/mL).
Chemical Information
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CAS. Nr. 174635-69-9
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Appearance Solid
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Molecular Weight 380.48
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Formel C26H24N2O
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Color White to off-white
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SMILES
O=C(C1=C(C)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Neuron
2026 Jan 8:S0896-6273(25)00927-4. PMID: 41512855 -
Adv Sci (Weinh)
2026 Feb 3:e16660. PMID: 41632021 -
Life Sci
Neurokinin 3 receptor antagonist-induced adipocyte activation improves obesity and metabolism in PCOS-like mice. [Abstract]2022 Dec 1:310:121078. PMID: 36252700 -
Am J Reprod Immunol
The overexpression of neurokinin B-neurokinin 3 receptor system exerts direct effects on the ovary under PCOS-like conditions to interfere with mitochondrial function. [Abstract]2023 Mar;89(3):e13663. PMID: 36453600 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (262.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL | 65.7065 mL |
| 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | 13.1413 mL | |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL | 6.5706 mL | |
| 15 mM | 0.1752 mL | 0.8761 mL | 1.7522 mL | 4.3804 mL | |
| 20 mM | 0.1314 mL | 0.6571 mL | 1.3141 mL | 3.2853 mL | |
| 25 mM | 0.1051 mL | 0.5257 mL | 1.0513 mL | 2.6283 mL | |
| 30 mM | 0.0876 mL | 0.4380 mL | 0.8761 mL | 2.1902 mL | |
| 40 mM | 0.0657 mL | 0.3285 mL | 0.6571 mL | 1.6427 mL | |
| 50 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL | 1.3141 mL | |
| 60 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0951 mL | |
| 80 mM | 0.0329 mL | 0.1643 mL | 0.3285 mL | 0.8213 mL | |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6571 mL |
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