2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. Didesmethyl cariprazine

Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.

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Didesmethyl cariprazine

Didesmethyl cariprazine Chemical Structure

CAS No. : 839712-25-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Didesmethyl cariprazine Related Antibodies

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Description

Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons[1][2].

IC50 & Target[2]

human 5-HT1A Receptor

1.7 nM (Ki)

Human D3 Receptor

0.056 nM (Ki)

D2L Receptor

1.41 nM (Ki)

human 5-HT2B Receptor

0.52 nM (Ki)

In Vitro

Didesmethyl cariprazine is a partial agonist of D2 and D3 receptors, a full agonist of the 5-HT1A receptor, and an antagonist of the human 5-HT2B receptor (Ki: 1.41 nM (human D2L)), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B))[2].

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

Didesmethyl cariprazine Related Antibodies
In Vivo

Didesmethyl cariprazine (120 μg/kg; i.v.) dose-dependently but partially suppresses the spontaneous activity of midbrain dopaminergic neurons in rats[2].

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

399.36

Formula

C19H28Cl2N4O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N)N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1
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
In Vitro: 

DMSO : 11.36 mg/mL (28.45 mM; ultrasonic and warming and heat to 80°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 2.5040 mL 12.5200 mL 25.0401 mL
5 mM 0.5008 mL 2.5040 mL 5.0080 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

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
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Working solution concentration: mg/mL
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. 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 2.5040 mL 12.5200 mL 25.0401 mL 62.6002 mL
5 mM 0.5008 mL 2.5040 mL 5.0080 mL 12.5200 mL
10 mM 0.2504 mL 1.2520 mL 2.5040 mL 6.2600 mL
15 mM 0.1669 mL 0.8347 mL 1.6693 mL 4.1733 mL
20 mM 0.1252 mL 0.6260 mL 1.2520 mL 3.1300 mL
25 mM 0.1002 mL 0.5008 mL 1.0016 mL 2.5040 mL
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Didesmethyl cariprazine Related Classifications

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.

Keywords:

Didesmethyl cariprazine839712-25-35-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorCariprazineD3D2receptor5-HT(1A)Inhibitorinhibitorinhibit

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