R-185
R-185 is an orally active and brain-penetrant GPR52 agonist. R-185 activates GPR52 to increase intracellular cAMP levels. R-185 can be used for the research of schizophrenia.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3066783-67-0
- 分子式: C22H19F4N5O2
- 分子量:461.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
| Species | Dose | Route | AUC0-∞ | T1/2 | Cmax | CL | Vd | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | p.o. | 3232 ng·h/mL | 1.76 h | 1173 ng/mL | / | / | 130 % |
| Mice[1] | 1 mg/kg | i.v. | 496 ng·h/mL | 1.40 h | 1283 ng/mL | 33.8 mL/min/kg | 1.74 L/kg | / |
| Rat[1] | 5 mg/kg | p.o. | 2284 ng·h/mL | 3.53 h | 318 ng/mL | / | 4.40 L/kg | 67 % |
| Rat[1] | 1 mg/kg | i.v. | 680 ng·h/mL | 2.05 h | 760 ng/mL | 24.8 mL/min/kg | / | / |
R-185 (1-5 mg/kg; p.o. or i.v.; single dose) exhibits favorable pharmacokinetic characteristics in mice, crosses the blood-brain barrier, and has an oral bioavailability of 130%[1].
R-185 (1-5 mg/kg; p.o. or i.v.; single dose) exhibits favorable pharmacokinetic characteristics in rats, crosses the blood-brain barrier, and has an oral bioavailability of 67%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD mice (male, 30 g)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:p.o. or i.v.; single dose
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Result:Exihibited favorable pharmacokinetic characteristics and could cross the blood-brain barrier.
Showed F of 130%, Cmax of 1173 ng/mL, Tmax of 1.76 h and AUC0-∞ of 3232 ng·h/mL (p.o.).
Showed T1/2 of 1.40 h, CL of 33.8 mL/min/kg, Vd of 1.74 L/kg and AUC0-∞ of 496 ng·h/mL (i.v.).
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Animal Model:SD rats (male, 200-250 g)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:p.o. or i.v.; single dose
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Result:Exihibited favorable pharmacokinetic characteristics and could cross the blood-brain barrier.
Exhibited F of 67%, Cmax of 318 ng/mL, Tmax of 3.53 h and AUC0-∞ of 2284 ng·h/mL (p.o.).
Exhibited T1/2 of 2.05 h, CL of 24.8 mL/min/kg, Vd of 4.4 L/kg and AUC0-∞ of 680 ng·h/mL (i.v.).
化学情報
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CAS 番号 3066783-67-0
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分子量 461.41
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分子式 C22H19F4N5O2
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SMILES
FC1=CC(OC2CCN(CC2)C3=C(N=CC=N3)C(NC4=CC=NC=C4)=O)=CC(C(F)(F)F)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
R-185 関連分類
HY-184192 関連分類
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