Cat. No.: HY-163763

T-10418

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T-10418 is a potent and highly selective G2A/GPR132 agonist. T-10418 has an EC₅₀ of 0.82 μM for human G2A activation. T-10418 has good water solubility, metabolic stability, and pharmacokinetic properties. T-10418 can be used for the research of various diseases such as neuropathic pain, acute myeloid leukemia, and inflammation.

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Pureté: 99.78%
CAS No.: 1608784-68-4
Formule: C₂₂H₂₀N₂O₄
Masse moléculaire:376.41

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

T-10418 Chemical Structure

CAS No.: 1608784-68-4

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

In Vitro

T-10418 (100 nM; 4 min) significantly enhances Capsaicin (HY-10448)-induced TRPV1 responses in primary mouse sensory neurons^[1].
T-10418 (30 μM; 72 h) does not affect the proliferation and viability of Molm13 and ML-2 acute myeloid leukemia cells^[1].

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

In Vivo

Pharmacokinetic Analysis in Male C57Bl/6N Mice^[1]

Route	Dose (mg/kg)	C_max (ng/mL)	T_max (h)	C_final (ng/mL)	CL/F [mL/(h·kg)]	CL [mL/(h·kg)]	AUC (ng·h/mL)
i.v.	1	45.3	15 min	2.4	16451	/	47.3
s.c.	10	755	30 min	2.9	/	8451	591

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

Chemical Information

CAS No. 1608784-68-4
Appearance Solid
Masse moléculaire 376.41
Formule C₂₂H₂₀N₂O₄
Color White to off-white
SMILES

O=C(C1=CC(OCC2=CN=CC=C2)=CC=C1)N[C@H](CC3=CC=CC=C3)C(O)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (265.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6567 mL

13.2834 mL

26.5668 mL

5 mM

0.5313 mL

2.6567 mL

5.3134 mL

10 mM

0.2657 mL

1.3283 mL

2.6567 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 5 mg/mL (13.28 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Hernandez-Olmos V, et al., Development of a Potent and Selective G2A (GPR132) Agonist. J Med Chem. 2024 Jun 25. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.6567 mL	13.2834 mL	26.5668 mL	66.4169 mL
	5 mM	0.5313 mL	2.6567 mL	5.3134 mL	13.2834 mL
	10 mM	0.2657 mL	1.3283 mL	2.6567 mL	6.6417 mL
	15 mM	0.1771 mL	0.8856 mL	1.7711 mL	4.4278 mL
	20 mM	0.1328 mL	0.6642 mL	1.3283 mL	3.3208 mL
	25 mM	0.1063 mL	0.5313 mL	1.0627 mL	2.6567 mL
	30 mM	0.0886 mL	0.4428 mL	0.8856 mL	2.2139 mL
	40 mM	0.0664 mL	0.3321 mL	0.6642 mL	1.6604 mL
	50 mM	0.0531 mL	0.2657 mL	0.5313 mL	1.3283 mL
	60 mM	0.0443 mL	0.2214 mL	0.4428 mL	1.1069 mL
	80 mM	0.0332 mL	0.1660 mL	0.3321 mL	0.8302 mL
	100 mM	0.0266 mL	0.1328 mL	0.2657 mL	0.6642 mL

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T-10418

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Highly Selective Activators Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

T-10418

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Highly Selective Activators Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

T-10418 Related Classifications

HY-163763 Related Classifications