2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Basmisanil

Basmisanil  (Synonyms: RG1662; RO5186582)

Cat. No.: HY-16716 Purity: 99.89%
COA Handling Instructions

Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.

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

Basmisanil Chemical Structure

Basmisanil Chemical Structure

CAS No. : 1159600-41-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 65 In-stock
10 mg USD 94 In-stock
50 mg USD 281 In-stock
100 mg USD 479 In-stock
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Based on 1 publication(s) in Google Scholar

Basmisanil Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Basmisanil

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders[1].

IC50 & Target

IC50: 8 nM (GABAAα5)
Ki: 5 nM (GABAAα5); 1031 nM (GABAAα1); 458 nM (GABAAα2); 510 nM (GABAAα3)
In Vitro

Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors[1].
Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM[1].
Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes[1].

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

Basmisanil Related Antibodies
In Vivo

Basmisanil (3-100 mg/kg, p.o.) occupies GABAA-α receptor in dose-dependent in rat brain[1].
Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects[1].

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

Animal Model: Sprague Dawley rats[1]
(180 g; female)
Dosage: 3-100 mg/kg
Administration: p.o.
Result: Decreased the binding of [3H]-Ro 15-4513 in a dose-dependent manner.
Reduced specific binding in the hippocampus by 70% at the highest dose (100 mg/kg).
Animal Model: Lister Hooded rats, Wistar rats and F-344 Fischer rats [1]
(Lister Hooded rats: 220-250 g; male)
(Wistar rats: 200-220 g; male and female)
(F-344 Fischer rats: 170-180 g; male)
Dosage: 3-600 mg/kg
Administration: p.o.
Result: Significantly attenuated the diazepam-induced deficit.
Showed plasma concentrations in dose- and time-dependent manner and reached a maximal level of 903 ng/mL (379 nM free plasma) 30 min after the administration at 10 mg/kg.
Animal Model: Male cynomolgus macaques[1]
(Macaca fascicularis; 7-10 kg)
Dosage: 1-600 mg/kg
Administration: p.o.
Result: Significantly improved the percentage of correct first reaches during difficult trials of the object retrieval task at the 3 and 10 mg/kg doses.
Exhibited an inverted U-shaped dose response in this paradigm with the 1 and 30 mg/kg doses producing no marked improvement on performance.
Increased the total plasma exposure in dose-dependent.
Clinical Trial
Molecular Weight

445.46

Appearance

Solid

Formula

C21H20FN3O5S
CAS No.
SMILES

O=C(N1CCS(CC1)(=O)=O)C2=CC=C(OCC3=C(C)ON=C3C4=CC=C(F)C=C4)N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (224.49 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2449 mL 11.2244 mL 22.4487 mL
5 mM 0.4490 mL 2.2449 mL 4.4897 mL
10 mM 0.2245 mL 1.1224 mL 2.2449 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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Basmisanil 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.

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Keywords:

Basmisanil1159600-41-5RG1662 RO5186582RG 1662RG-1662RO5186582RO 5186582RO-5186582GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα subunit-containing GABAA receptors (GABAAα5)negative allosteric modulator (NAMs)cognitivepsychiatric disordersInhibitorinhibitorinhibit

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