1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. CP-809101 hydrochloride

CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.

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CP-809101 hydrochloride Chemical Structure

CP-809101 hydrochloride Chemical Structure

CAS No. : 1215721-40-6

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Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
USD 162 In-stock
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10 mM * 1 mL in Water USD 162 In-stock
Solid
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10 mg USD 147 In-stock
50 mg USD 634 In-stock
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Description

CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence[1][2].

IC50 & Target

5-HT2C Receptor

9.96 (pEC50)

5-HT2B Receptor

7.19 (pEC50)

5-HT2A Receptor

6.81 (pEC50)

In Vivo

CP-809101 hydrochloride (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner[1].
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner)[1].
CP-809101 hydrochloride (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED50 value of 2.2 mg/kg[1].
CP-809101 hydrochloride (0.3, 1, 3 mg/kg; s.c.; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine[2].

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

Animal Model: Male CF rats (conditioned avoidance responding (CAR) model)[1].
Dosage: 0.1-56 mg/kg
Administration: Subcutaneous injection; single.
Result: Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg.
Animal Model: Male CD rats (PCP or d-amphetamine-induced hyperactivity model)[1].
Dosage: 0.56, 1.78, 5.6, 17.8 mg/kg
Administration: Subcutaneous injection; single.
Result: Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg.
Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner.
Animal Model: Male CD rats (spontaneous locomotor model)[1].
Dosage: 0.56, 1.78, 5.6, 17.8 mg/kg
Administration: Subcutaneous injection; single.
Result: Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg).
Animal Model: Adult male Sprague-Dawley rats (280-400 g)[2].
Dosage: 0.3, 1, 3 mg/kg
Administration: Subcutaneous injection; single.
Result: Produced a dose-related decrease in responding for food and nicotine self-administration in rats.
Molecular Weight

341.24

Formula

C15H18Cl2N4O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Cl.ClC1=CC(COC2=NC(N3CCNCC3)=CN=C2)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 20 mg/mL (58.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9305 mL 14.6524 mL 29.3049 mL
5 mM 0.5861 mL 2.9305 mL 5.8610 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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 (sealed storage, away from moisture). 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
H2O 1 mM 2.9305 mL 14.6524 mL 29.3049 mL 73.2622 mL
5 mM 0.5861 mL 2.9305 mL 5.8610 mL 14.6524 mL
10 mM 0.2930 mL 1.4652 mL 2.9305 mL 7.3262 mL
15 mM 0.1954 mL 0.9768 mL 1.9537 mL 4.8841 mL
20 mM 0.1465 mL 0.7326 mL 1.4652 mL 3.6631 mL
25 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9305 mL
30 mM 0.0977 mL 0.4884 mL 0.9768 mL 2.4421 mL
40 mM 0.0733 mL 0.3663 mL 0.7326 mL 1.8316 mL
50 mM 0.0586 mL 0.2930 mL 0.5861 mL 1.4652 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    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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CP-809101 hydrochloride
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