2. GPCR/G Protein
  3. P2Y Receptor
  4. AZD1283

AZD1283 is a potent P2Y12 receptor antagonist with a binding IC50 of 11 nM and a GTPγS IC50 of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders.

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

AZD1283 Chemical Structure

AZD1283 Chemical Structure

CAS No. : 919351-41-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 93 In-stock
Solution
10 mM * 1 mL in DMSO USD 93 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 155 In-stock
50 mg USD 430 In-stock
100 mg USD 730 In-stock
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Based on 1 publication(s) in Google Scholar

AZD1283 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD1283 is a potent P2Y12 receptor antagonist with a binding IC50 of 11 nM and a GTPγS IC50 of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders[1][2].

IC50 & Target[1]

P2Y12 Receptor

11 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.011 μM
Compound: 3, AZD1283
Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis
Displacement of [125I]-AZ11931285 from P2Y12 receptor (unknown origin) expressed in CHO cell membrane after 1 hr by scintillation counting analysis
[PMID: 23899349]
CHO IC50
0.025 μM
Compound: 3, AZD1283
Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay
Antagonist activity at P2Y12 receptor (unknown origin) expressed in CHO cell membrane by [35S]GTPgammaS binding assay
[PMID: 23899349]
CHO-K1 IC50
14 nM
Compound: 1
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 seconds
[PMID: 24835983]
CHO-K1 IC50
22 nM
Compound: 1
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 30 seconds
[PMID: 24835983]
CHO-K1 IC50
44 nM
Compound: 1
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds
[PMID: 24835983]
CHO-K1 IC50
9 nM
Compound: 1
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 60 mins
[PMID: 24835983]
In Vitro

AZD1283 exhibits excellent antiplatelet aggregation potency with an IC50 value of 3.6 μM[1].
AZD1283 has highly inhibitory activity against CYP450 with IC50 values of 6.62 μM, 0.399 μM and 4.28 μM and 3.64 μM for CYP2C9, CYP2C19, CYP3A4 (Midazolam as the substrate) and CYP3A4 (Testosterone as the substrate), respectively[1].
AZD1283 induces increases in blood flow and inhibition of ADP-induced platelet aggregation with an antithrombotic EC50 value of 3 μg/(kg×min)[2].

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

AZD1283 Related Antibodies
In Vivo

AZD1283 exhibits poor liver microsomal stability in rat (T1/2 = 6.08 min), but better in dog microsomes (T1/2 = 201 min) and human microsomes (T1/2 = 65.0 min)[1].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 5 mg/kg
Administration: p.o.; single dosage
Result: Exhibited a Cmax of 25.9 ± 11 ng/mL, a T1/2 of 1.68 ± 0.37 h and a Tmax of 0.25 h.
Molecular Weight

470.54

Formula

C23H26N4O5S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC1=C(C(OCC)=O)C=C(C#N)C(N2CCC(C(NS(=O)(CC3=CC=CC=C3)=O)=O)CC2)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (212.52 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 2.1252 mL 10.6261 mL 21.2522 mL
5 mM 0.4250 mL 2.1252 mL 4.2504 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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 (5.31 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.

    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: ≥ 2.5 mg/mL (5.31 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

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

Purity: 99.33%

SDS (393 KB)

COA (252 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1252 mL 10.6261 mL 21.2522 mL 53.1304 mL
5 mM 0.4250 mL 2.1252 mL 4.2504 mL 10.6261 mL
10 mM 0.2125 mL 1.0626 mL 2.1252 mL 5.3130 mL
15 mM 0.1417 mL 0.7084 mL 1.4168 mL 3.5420 mL
20 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6565 mL
25 mM 0.0850 mL 0.4250 mL 0.8501 mL 2.1252 mL
30 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7710 mL
40 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.3283 mL
50 mM 0.0425 mL 0.2125 mL 0.4250 mL 1.0626 mL
60 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
80 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6641 mL
100 mM 0.0213 mL 0.1063 mL 0.2125 mL 0.5313 mL
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AZD1283 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:

AZD1283919351-41-0AZD 1283AZD-1283P2Y Receptorantiplatelet aggregationthromboembolicantithromboticInhibitorinhibitorinhibit

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