2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. A-437203

A-437203  (Synonyms: Lu201640; A37203)

Cat. No.: HY-U00185 Purity: 99.08%
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A-437203 is a selective D3 receptor antagonist with Ki of 71, 1.6, and 6220 nM for D2, D3, and D4 receptors, respectively.

For research use only. We do not sell to patients.

A-437203 Chemical Structure

A-437203 Chemical Structure

CAS No. : 220519-06-2

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A-437203 Related Antibodies

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  • Protocol

  • Purity & Documentation

  • References

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Description

A-437203 is a selective D3 receptor antagonist with Ki of 71, 1.6, and 6220 nM for D2, D3, and D4 receptors, respectively.

IC50 & Target

Ki :71 nM (D2 receptor), 1.6 nM (D3 receptor), 6220 nM (D4 receptor)[1]
In Vitro

A-437203 is an antagonist with high affinity for D3 receptors and relatively high selectivity compared to other dopamine receptor subtypes (44-fold selective for D3 vs D2)[1].

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

A-437203 Related Antibodies
In Vivo

A-437203, a selective D3 receptor antagonist, is initially tested alone in rat forced swim test (FST). Doses of A-437203 evaluated are 0.52, 1.75, 5.24, and 17.46 μmol/kg i.p. Doses are chosen based on the selectivity of A-437203 for D3 vs D2 dopamine receptors and reports indicating that the effects of A-437203 at doses of 17.46 μmol/kg (10 mg/kg) or lower are clearly mediated by D3 but not D2 receptors, since higher doses of the compound such as 174.6 μmol/kg (100 mg/kg) are necessary to bind and block D2 receptor from the irreversible inactivation induced by the alkylating agent EEDG. ANOVA revealed no significant difference between the treatments for any of the behaviors analyzed (F4, 45=1.12, p=0.359 for immobility, F4, 45=0.188, p=0.943 for climbing, and F4, 45=1.634, p=0.182 for swimming). Based on these results, the dose of 17.46 μmol/kg i.p. of A-437203 is selected for further experiments[1].

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

456.53

Formula

C20H27F3N6OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC(SCCCN2CCN(C3=NC(C(C)(C)C)=NC(C(F)(F)F)=C3)CC2)=NC=C1
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 : ≥ 125 mg/mL (273.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1904 mL 10.9522 mL 21.9044 mL
5 mM 0.4381 mL 2.1904 mL 4.3809 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

Rats[1]
Male Sprague-Dawley rats weighing 250-350 g are used for these experiments. Haloperidol (0.27, 1.33, and 2.66 μmol/kg=0.1, 0.5, and 1.0 mg/kg i.p.), A-437203 (LU-201640) (0.52, 1.75, 5.24, and 17.46 μmol/kg=0.3, 1.0, 3.0, and 10.0 mg/kg i.p.), and L-745,870 (0.23, 1.15, 2.3, and 5.7 μmol/kg=0.1, 0.5, 1.0, and 2.5 mg/kg i.p.) are tested initially alone in order to determine effective dose ranges. In those experiments, haloperidol, A-437203, and L-745,870 are administered i.p. 24, 5, and 0.5 h before the test swim. In the subsequent antagonism experiments, Haloperidol (0.27 μmol/kg), A-437203 (17.46 μmol/kg) or L-745,870 (1.15 μmol/kg) are injected i.p. 15 min prior to each quinpirole injection (0.4 and 1.0 μmol/kg s.c.).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 2.1904 mL 10.9522 mL 21.9044 mL 54.7609 mL
5 mM 0.4381 mL 2.1904 mL 4.3809 mL 10.9522 mL
10 mM 0.2190 mL 1.0952 mL 2.1904 mL 5.4761 mL
15 mM 0.1460 mL 0.7301 mL 1.4603 mL 3.6507 mL
20 mM 0.1095 mL 0.5476 mL 1.0952 mL 2.7380 mL
25 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1904 mL
30 mM 0.0730 mL 0.3651 mL 0.7301 mL 1.8254 mL
40 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3690 mL
50 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
60 mM 0.0365 mL 0.1825 mL 0.3651 mL 0.9127 mL
80 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6845 mL
100 mM 0.0219 mL 0.1095 mL 0.2190 mL 0.5476 mL
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A-437203 Related Classifications

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  • 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:

A-437203220519-06-2Lu201640 A37203A437203A 437203Lu 201640Lu-201640A37203A 37203A-37203Dopamine ReceptorInhibitorinhibitorinhibit

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