2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Amelparib

Amelparib  (Synonyms: JPI-289 free base)

Cat. No.: HY-116218 Purity: 99.17%
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Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50=18.5 nM) and cellular PAR formation (IC50=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke.

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

Amelparib Chemical Structure

Amelparib Chemical Structure

CAS No. : 1227156-72-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 929 In-stock
Solution
10 mM * 1 mL in DMSO USD 929 In-stock
Solid
1 mg USD 490 In-stock
5 mg USD 1230 In-stock
10 mg USD 1980 In-stock
25 mg USD 3980 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Amelparib:

Amelparib Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50=18.5 nM) and cellular PAR formation (IC50=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke[1].

IC50 & Target

IC50: 18.5 nM (PARP-1)[1].
In Vitro

Amelparib (0.001 mM-1 mM; 2 h) dose-dependently reduces the number of apoptotic cells in cortical neurons induced by hypoxia for 24 h and 48 h[1].
Amelparib (0, 0.01, 0.1 and 1 mM; 2 h) dose-dependently reduces the increased PARP activity in cortical neurons, the expression of cleaved caspase-3 in cortical neurons subjected to 6 h of hypoxia, and the levels of HIF-1α and PAR in cortical neurons subjected to 2 h of hypoxia[1].

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

Amelparib Related Antibodies

Apoptosis Analysis[1]

Cell Line: PCCNs
Concentration: 0.001-1 mM
Incubation Time: 2 h
Result: Reduces apoptosis of PCCNs induced by hypoxia for 24h and 48h dose-dependently.

Western Blot Analysis[1]

Cell Line: PCCNs
Concentration: 0, 0.01, 0.1 and 1 mM
Incubation Time: 2 h
Result: Decreased the levels of HIF-1α, PAR, AIF, and cytochrome c at 2 h of administration dose-dependently.
Reduced the expression of cleaved caspase-3 in the case of 6 h administration dose-dependently.
In Vivo

Amelparib (5, 7.5 and 10 mg/kg, i.v.; single dose) reduces infarct volume in rats with transient and permanent MCAO models by 30% and 53%, respectively, at a dose of 7.5 or 10 mg/kg[2].
Amelparib (10 mg/kg, i.v.; single dose 2 or 8 h after MCAO) reduces mean infarct size and alleviates brain swelling in male SD rats[2].
Amelparib (10 mg/kg, i.v.; single dose 2 h after MCAO) reduces apoptosis of penumbra cells in male SD rats[2].

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

Animal Model: Male Sprague–Dawley rats[2]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), 2 h after MCAO
Result: Reduced the infarct area by 53% and the number of apoptotic cells by 56% after 24 h of administration.
Clinical Trial
Molecular Weight

343.42

Formula

C19H25N3O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C2=C(C3=C(C=C(C=C3N1)CN4CCOCC4)OCC)NCCC2
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 (291.19 mM; ultrasonic and adjust pH to 2 with 1M HCl; 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 2.9119 mL 14.5594 mL 29.1189 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 2.5 mg/mL (7.28 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.28 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9119 mL 14.5594 mL 29.1189 mL 72.7972 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL 14.5594 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 mL 7.2797 mL
15 mM 0.1941 mL 0.9706 mL 1.9413 mL 4.8531 mL
20 mM 0.1456 mL 0.7280 mL 1.4559 mL 3.6399 mL
25 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9119 mL
30 mM 0.0971 mL 0.4853 mL 0.9706 mL 2.4266 mL
40 mM 0.0728 mL 0.3640 mL 0.7280 mL 1.8199 mL
50 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4559 mL
60 mM 0.0485 mL 0.2427 mL 0.4853 mL 1.2133 mL
80 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9100 mL
100 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7280 mL
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Amelparib Related Classifications

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:

Amelparib1227156-72-0JPI-289JPI289JPI 289PARPpoly ADP ribose polymeraseoralwater-solublePARP-1PAR formationneuroprotectiveacute ischaemic strokeInhibitorinhibitorinhibit

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