Referencia número: HY-151483

TK-129

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Based on 1 Customer Validation

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC₅₀=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.

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Pureza: ≥98.0%
No. CAS: 3031476-73-7
Fòrmula: C₁₅H₂₃N₅O₂
Peso molecular:305.38

Almacenamiento:

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

TK-129 Chemical Structure

No. CAS: 3031476-73-7

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

KDM5

44 nM (IC₅₀)

Ver todos los productos específicos de isoformas Wnt :

Ver todos los productos específicos de isoformas Histone Demethylase :

In Vitro

TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro^[1].
TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs^[1].
TK-129 (0.1, 0.2, 0.3, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

NRCFs and NRCMs
Concentration:

10 μM
Incubation Time:

48 h
Result:

Exhibited the cell survival rates were almost more than 90%.

Western Blot Analysis^[1]

Cell Line:

NRCFs
Concentration:

0.1, 0.2, 0.3, 0.4, 0.5 μM
Incubation Time:

48 h
Result:

Increased the expression level of KDM5B substrate H3K4me3 protein in a concentration-dependent manner.

In Vivo

TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice^[1].
TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo^[1].
TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo^[1].

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

Animal Model:

Wild C57BL/6 mice (8 to 10-week-old; half male and half female)^[1].
Dosage:

2 g/kg
Administration:

Oral gavage, single.
Result:

Exhibited all mice in the acute toxicity group survived and gained weight normally, after 2 weeks.

Animal Model:

C57BL/6 mice (isoproterenol (ISO)-induced)^[1].
Dosage:

50 mg/kg
Administration:

Oral gavage, twice daily for 24 days.
Result:

Alleviated myocardial remodeling induced by ISO in vivo.

Animal Model:

Male SD Rats (223.5-265.1 g)^[1].
Dosage:

2 mg/kg (for i.v.); 10 mg/kg (for p.o.).
Administration:

Intravenous injection or oral gavage; single.

Result:

1.19 Pharmacokinetic Parameters of TK-129 in Male SD Rats^[1].

	PO (10 mg/kg)	IV (2 mg/kg)
CL (L/h/kg)	9.9	4.2
V_ss (L/kg)	33.4	2.7
T_1/2 (h)	2.4	0.4
T_max (h)	0.4	-
C_max (ng/mL)	709.7	1229.1
AUC_0-24 (ng/mL•h)	1038.2	479.6
F (%)	42.37	-

Chemical Information

No. CAS 3031476-73-7
Appearance Solid
Peso molecular 305.38
Fòrmula C₁₅H₂₃N₅O₂
Color White to off-white
SMILES

O=C(N[C@H]1CN(C(C2=NNC(C(C)C)=C2)=O)CC1)NC3CC3
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (327.46 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

3.2746 mL

16.3730 mL

32.7461 mL

5 mM

0.6549 mL

3.2746 mL

6.5492 mL

10 mM

0.3275 mL

1.6373 mL

3.2746 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Tang K, et al. Discovery of Novel Pyrazole-Based KDM5B Inhibitor TK-129 and Its Protective Effects on Myocardial Remodeling and Fibrosis. J Med Chem. 2022 Sep 16. [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	3.2746 mL	16.3730 mL	32.7461 mL	81.8652 mL
	5 mM	0.6549 mL	3.2746 mL	6.5492 mL	16.3730 mL
	10 mM	0.3275 mL	1.6373 mL	3.2746 mL	8.1865 mL
	15 mM	0.2183 mL	1.0915 mL	2.1831 mL	5.4577 mL
	20 mM	0.1637 mL	0.8187 mL	1.6373 mL	4.0933 mL
	25 mM	0.1310 mL	0.6549 mL	1.3098 mL	3.2746 mL
	30 mM	0.1092 mL	0.5458 mL	1.0915 mL	2.7288 mL
	40 mM	0.0819 mL	0.4093 mL	0.8187 mL	2.0466 mL
	50 mM	0.0655 mL	0.3275 mL	0.6549 mL	1.6373 mL
	60 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3644 mL
	80 mM	0.0409 mL	0.2047 mL	0.4093 mL	1.0233 mL
	100 mM	0.0327 mL	0.1637 mL	0.3275 mL	0.8187 mL

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TK-129

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Ver todos los productos específicos de isoformas Wnt

Ver todos los productos específicos de isoformas Histone Demethylase

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

TK-129 Related Classifications

HY-151483 Related Classifications