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CRK12-IN-1

Name: CRK12-IN-1
Brand: TargetMol
SKU: T63059
Price: 210 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T63059Cas No. 1990479-14-5

CRK12-IN-1 is a potent CRK12 inhibitor with insecticidal activity and exhibits inhibitory effects on Trypanosoma brucei (T.b. brucei) and Trypanosoma congolense (T. congolense) with EC50s of 1.3 and 18 nM, respectively, rapidly killing the pathogenic cells.

CRK12-IN-1

🥰Excellent

Purity: 99.72%

Catalog No. T63059Cas No. 1990479-14-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$210	In Stock	In Stock
5 mg	$497	In Stock	In Stock
10 mg	$678	In Stock	In Stock
25 mg	$953	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Batch Information

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Purity:99.72%

Appearance:Solid

Color:White

Resource Download

COA FNMR HNMR HPLC

Product Introduction

Bioactivity

Description	CRK12-IN-1 is a potent CRK12 inhibitor with insecticidal activity and exhibits inhibitory effects on Trypanosoma brucei (T.b. brucei) and Trypanosoma congolense (T. congolense) with EC50s of 1.3 and 18 nM, respectively, rapidly killing the pathogenic cells.
Targets&IC50	T. congolense:1.3 nM, T. vivax:18 nM
In vitro	CRK12-IN-1(compound 1) (10 mg/mL; 69 h) demonstrates exceptional potency against T.b. brucei, proving highly effective in animal models of T.b. brucei infection. Additionally, it serves as a potent inhibitor of T. congolensei, with EC50 values of 1.3 and 18 nM, respectively.[1]
In vivo	CRK12-IN-1 (compound 1) demonstrates moderate blood clearance and a short half-life (~1.8 h) in male ruminating Holstein-Friesian cattle, penetrating tissues beyond the vasculature (5 mg free base/kg, i.m. or 2.5 mg free base/kg, i.v.; 0.25-120 h). It reduces parasitemia in T. congolense-infected calves but does not prevent re-emergence after treatment ends (5 mg/kg, s.c., twice 12 h apart for 4 days). In female NMRI mice, CRK12-IN-1 shows 74% bioavailability and a half-life of ~1 h (10 mg free base/kg, s.c., 0.08-8 h). It achieves sterile cure against T. congolense in mice (50 or 10 mg/kg, s.c., once daily for 4 days) and is slightly more efficacious against T. vivax-infected mice (30 or 3 mg/kg, s.c., daily for 4 days).

Chemical Properties

Molecular Weight	472.57
Formula	C₂₀H₂₆F₂N₄O₃S₂
Cas No.	1990479-14-5
Smiles	C(=O)(C=1SC(N[C@@H]2CC[C@@H](NS(CC(C)C)(=O)=O)CC2)=NC1N)C3=C(F)C=CC=C3F

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (126.97 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1161 mL	10.5804 mL	21.1609 mL	105.8044 mL
5 mM	0.4232 mL	2.1161 mL	4.2322 mL	21.1609 mL
10 mM	0.2116 mL	1.0580 mL	2.1161 mL	10.5804 mL
20 mM	0.1058 mL	0.5290 mL	1.0580 mL	5.2902 mL
50 mM	0.0423 mL	0.2116 mL	0.4232 mL	2.1161 mL
100 mM	0.0212 mL	0.1058 mL	0.2116 mL	1.0580 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc