RIP1 kinase inhibitor 1

Name: RIP1 kinase inhibitor 1
Brand: MedChemExpress
SKU: HY-111409
Rating: 4.5 (1 reviews)

Cat. No.: HY-111409 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pK_i=9.04).

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

RIP1 kinase inhibitor 1 Chemical Structure

CAS No. : 2095515-38-9

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
50 mg	USD 1900	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pK_i=9.04)^[1].

IC₅₀ & Target

pKi: 9.04 (RIP1 kinase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	2 nM Compound: 22	Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity	[PMID: 29485864]
L929	IC₅₀	15 nM Compound: 22	Induction of necroptosis in mouse L929 cells assessed as increase in TNFalpha/zVAD-FMK-induced LDH release preincubated for 30 mins followed by TNFalpha/zVAD-FMK addition measured after 4 hrs by CytoTox 96 nonradioactive cytotoxicity assay Induction of necroptosis in mouse L929 cells assessed as increase in TNFalpha/zVAD-FMK-induced LDH release preincubated for 30 mins followed by TNFalpha/zVAD-FMK addition measured after 4 hrs by CytoTox 96 nonradioactive cytotoxicity assay	[PMID: 29485864]

In Vitro

RIP1 kinase inhibitor 1 (compound 22) strongly suppresses necroptotic cell death and phosphorylation of MLKL(pMLKL) in human colorectal adenocarcinoma HT-29 cells (nectoptosis, IC₅₀=2 nM; pMLKL, IC₅₀=1.3 nM) as well as mouse L-cells NCTC 929 (nectoptosis, IC₅₀=15 nM; pMLKL, IC₅₀=2.7 nM)^[1].

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

Molecular Weight

461.90

Formula

C₂₄H₂₀ClN₅O₃

CAS No.

2095515-38-9

Appearance

Solid

Color

White to yellow

SMILES

N#CC1=CC=C2N(C)C([C@@H](N3CCC4=C(Cl)N(CC5=CC=CC=C5)N=C4C3=O)COC2=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (432.99 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	2.1650 mL	10.8249 mL	21.6497 mL
5 mM	0.4330 mL	2.1650 mL	4.3299 mL
10 mM	0.2165 mL	1.0825 mL	2.1650 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 (sealed storage, away from moisture and light). 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:

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

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: 5 mg/mL (10.82 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (10.82 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

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Yoshikawa M, et al. Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, OrallyAvailable, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships. J Me [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1650 mL	10.8249 mL	21.6497 mL	54.1243 mL
	5 mM	0.4330 mL	2.1650 mL	4.3299 mL	10.8249 mL
	10 mM	0.2165 mL	1.0825 mL	2.1650 mL	5.4124 mL
	15 mM	0.1443 mL	0.7217 mL	1.4433 mL	3.6083 mL
	20 mM	0.1082 mL	0.5412 mL	1.0825 mL	2.7062 mL
	25 mM	0.0866 mL	0.4330 mL	0.8660 mL	2.1650 mL
	30 mM	0.0722 mL	0.3608 mL	0.7217 mL	1.8041 mL
	40 mM	0.0541 mL	0.2706 mL	0.5412 mL	1.3531 mL
	50 mM	0.0433 mL	0.2165 mL	0.4330 mL	1.0825 mL
	60 mM	0.0361 mL	0.1804 mL	0.3608 mL	0.9021 mL
	80 mM	0.0271 mL	0.1353 mL	0.2706 mL	0.6766 mL
	100 mM	0.0216 mL	0.1082 mL	0.2165 mL	0.5412 mL