1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB228357

SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.

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SB228357

SB228357 構造式

CAS 番号 : 181629-93-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 143 在庫あり
Solution
10 mM * 1 mL in DMSO USD 143 在庫あり
Solid
5 mg $130 在庫あり
10 mg $200 在庫あり
25 mg $400 在庫あり
50 mg $650 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects[1][2].

IC50 & Target[1]

5-HT2A Receptor

 

5-HT2B Receptor

 

5-HT2C Receptor

 

5-HT2A Receptor

6.9 (pKi)

5-HT2C Receptor

9 (pKi)

5-HT2B Receptor

8 (pKi)

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
0.01 3
Compound: 2
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
[PMID: 24900481]
CHO-K1 IC50
0.01 3
Compound: 2
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
[PMID: 24900481]
CHO-K1 IC50
0.01 3
Compound: 2
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
[PMID: 24900481]
体内実験

SB228357 (0-10 mg/kg; oral administration; for 90 minutes; male Sprague Dawley rats) treatment significantly reverses Haloperidol-induced catalepsy[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley rats (200-250 g) injected with Haloperidol[2]
Dosage: 0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg
Administration: Oral administration; for 90 minutes
Result: Significantly reversed Haloperidol-induced catalepsy.
分子量

431.38

分子式

C22H17F4N3O2

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC2=C1C=C(C(F)(F)F)C(OC)=C2)NC3=CC(C4=CC=CN=C4)=CC(F)=C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (289.77 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3181 mL 11.5907 mL 23.1814 mL
5 mM 0.4636 mL 2.3181 mL 4.6363 mL
10 mM 0.2318 mL 1.1591 mL 2.3181 mL
View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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一般には略語で表示されます:C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 99.43%

参考文献

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3181 mL 11.5907 mL 23.1814 mL 57.9535 mL
5 mM 0.4636 mL 2.3181 mL 4.6363 mL 11.5907 mL
10 mM 0.2318 mL 1.1591 mL 2.3181 mL 5.7954 mL
15 mM 0.1545 mL 0.7727 mL 1.5454 mL 3.8636 mL
20 mM 0.1159 mL 0.5795 mL 1.1591 mL 2.8977 mL
25 mM 0.0927 mL 0.4636 mL 0.9273 mL 2.3181 mL
30 mM 0.0773 mL 0.3864 mL 0.7727 mL 1.9318 mL
40 mM 0.0580 mL 0.2898 mL 0.5795 mL 1.4488 mL
50 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1591 mL
60 mM 0.0386 mL 0.1932 mL 0.3864 mL 0.9659 mL
80 mM 0.0290 mL 0.1449 mL 0.2898 mL 0.7244 mL
100 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5795 mL
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  • Molarity Calculator

  • Dilution Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
SB228357
製品番号:
HY-103154
数量:
MCE 日本正規代理店: