TGFBR1-IN-2

Cat. No.: HY-164793: FAQs
Data Sheet Handling Instructions

Molarity Calculator

TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.

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

TGFBR1-IN-2 Chemical Structure

CAS No. : 733806-89-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 423	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 423	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 385	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 656	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1480	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3220	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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•Related Small Molecules:

•Related Proteins:

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms

ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

TGFBR1

0.01 μM (Kd)

In Vitro

TGFBR1-IN-2 inhibits nonreplicating Mycobacterium tuberculosis, with MIC_90NR of 1 μM, MIC₉₀ of 20 μM, MIC₅₀ of 16 μM^[1].
TGFBR1-IN-2 (2-20 μM, 35 days) inhibits drug-tolerant microorganisms (Mycobacterium tuberculosis-GFP culture with Rifampicin (HY-B0272) and Isoniazid (HY-B0329))^[1].

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

Cell Viability Assay^[1]

Cell Line:	an Mtb-GFP culture with Rifampicin and Isoniazid
Concentration:	2, 20 μM
Incubation Time:	35 days
Result:	Showed full activity against Mtb-GFP (at 2 μM and 20 μM).

In Vivo

TGFBR1-IN-2 (10 mg/kg. p.o.) demonstrates a short half-life and low plasma concentration in CD1 mice, with T_1/2 of 1.8 h, C_max of 280 ng/ mL and AUC_last of 640 h*ng/mL^[1].

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

Molecular Weight

313.36

Formula

C₁₉H₁₅N₅

CAS No.

733806-89-8

Appearance

Solid

SMILES

CC1=NC(C2=NC(NC3=CC=NC=C3)=C4C=CC=CC4=N2)=CC=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 : 100 mg/mL (319.12 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	3.1912 mL	15.9561 mL	31.9122 mL
5 mM	0.6382 mL	3.1912 mL	6.3824 mL
10 mM	0.3191 mL	1.5956 mL	3.1912 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

Handling Instructions (2659 KB)

References

[1]. Nandakumar, et al. Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline. Journal of medicinal chemistry. 2023, 66(21):14724-14734. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.1912 mL	15.9561 mL	31.9122 mL	79.7804 mL
	5 mM	0.6382 mL	3.1912 mL	6.3824 mL	15.9561 mL
	10 mM	0.3191 mL	1.5956 mL	3.1912 mL	7.9780 mL
	15 mM	0.2127 mL	1.0637 mL	2.1275 mL	5.3187 mL
	20 mM	0.1596 mL	0.7978 mL	1.5956 mL	3.9890 mL
	25 mM	0.1276 mL	0.6382 mL	1.2765 mL	3.1912 mL
	30 mM	0.1064 mL	0.5319 mL	1.0637 mL	2.6593 mL
	40 mM	0.0798 mL	0.3989 mL	0.7978 mL	1.9945 mL
	50 mM	0.0638 mL	0.3191 mL	0.6382 mL	1.5956 mL
	60 mM	0.0532 mL	0.2659 mL	0.5319 mL	1.3297 mL
	80 mM	0.0399 mL	0.1995 mL	0.3989 mL	0.9973 mL
	100 mM	0.0319 mL	0.1596 mL	0.3191 mL	0.7978 mL

TGFBR1-IN-2 Related Classifications

Infection

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:

TGFBR1-IN-2733806-89-8TGF-β ReceptorCytochrome P450BacterialTransforming growth factor beta receptorsCYPsMycobacterium tuberculosisMtbTuberculosisP450 metabolismPyridyl-6-methylMetabolic StabilityAntibacterialFibrosisInhibitorinhibitorinhibit

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