TPA-023B

Cat. No.: HY-19505 Purity: 98.58%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

TPA-023B is a high-affinity and orally active GABA_A receptor α2/α3 subtype (K_is of 0.73 nM/2 nM) partial agonist and a α1 subtype (K_i of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.

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

TPA-023B Chemical Structure

CAS No. : 425377-76-0

Size	Price	Stock	Quantity
5 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Description

In Vitro

TPA-023B also has high affinity for α5 subtype (K_i of 1.1 nM) of human recombinant GABA_A receptor, but over 1500-fold lower for the α4- and α6 containing subtypes (K_i > 1000 nM). TPA-023B also has a comparable affinity for native rat GABA_A receptors in different regions of the CNS (K_i of 0.32-0.99 nM in cerebellum, spinal cord and frontal cortex)^[1].
TPA-023B antagonizes the ability of chlordiazepoxide to potentiate the GABA EC₂₀-induced current in cells expressing the α1 subtype. More specifically, 3 μM chlordiazepoxide potentiates the GABA EC₂₀ current by 105% and this effect could be reduced to 8% in the presence of 100 nM TPA-023B^[1].

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

In Vivo

TPA-023B gives dose- and time-dependent occupancy of rat brain GABA_A receptors as measured using an in vivo [³H]flumazenil binding assay, with 50% occupancy corresponding to a respective dose and plasma drug concentration of 0.09 mg/kg and 19 ng/mL^[1].
TPA-023B is anxiolytic in rodent and primate (squirrel monkey) models of anxiety (elevated plus maze, fear-potentiated startle, conditioned suppression of drinking, conditioned emotional response) yet has no significant effects in rodent or primate assays of ataxia and/or myorelaxation (rotarod, chain-pulling, lever pressing), up to doses (10 mg/kg) corresponding to occupancy of greater than 99%^[1].

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

Molecular Weight

391.37

Formula

C₂₁H₁₅F₂N₅O

CAS No.

425377-76-0

Appearance

Solid

Color

Light yellow to green yellow

SMILES

N#CC1=CC=CC(F)=C1C2=CC(C3=CN=C4N3N=CC(C(C)(O)C)=N4)=CC=C2F

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 : 100 mg/mL (255.51 mM; Need ultrasonic; 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	2.5551 mL	12.7756 mL	25.5513 mL
5 mM	0.5110 mL	2.5551 mL	5.1103 mL
10 mM	0.2555 mL	1.2776 mL	2.5551 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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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

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

Purity: 98.58%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (255 KB) HNMR (211 KB) RP-HPLC (164 KB)

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5551 mL	12.7756 mL	25.5513 mL	63.8782 mL
	5 mM	0.5110 mL	2.5551 mL	5.1103 mL	12.7756 mL
	10 mM	0.2555 mL	1.2776 mL	2.5551 mL	6.3878 mL
	15 mM	0.1703 mL	0.8517 mL	1.7034 mL	4.2585 mL
	20 mM	0.1278 mL	0.6388 mL	1.2776 mL	3.1939 mL
	25 mM	0.1022 mL	0.5110 mL	1.0221 mL	2.5551 mL
	30 mM	0.0852 mL	0.4259 mL	0.8517 mL	2.1293 mL
	40 mM	0.0639 mL	0.3194 mL	0.6388 mL	1.5970 mL
	50 mM	0.0511 mL	0.2555 mL	0.5110 mL	1.2776 mL
	60 mM	0.0426 mL	0.2129 mL	0.4259 mL	1.0646 mL
	80 mM	0.0319 mL	0.1597 mL	0.3194 mL	0.7985 mL
	100 mM	0.0256 mL	0.1278 mL	0.2555 mL	0.6388 mL

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:

TPA-023B425377-76-0Inhibitorinhibitorinhibit

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