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AZD1283 (Synonyms: AZD 1283, 6-4-(Benzylsulfonyl)aminocarbonylpiperidin-1-yl-5-cyano-2-methylnicotinic acid ethyl ester)

Catalog No.GC14956

Potent P2Y12 antagonist

Products are for research use only. Not for human use. We do not sell to patients.

AZD1283 Chemical Structure

Cas No.: 919351-41-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$118.00
In stock
5mg
$103.00
In stock
10mg
$179.00
In stock
50mg
$440.00
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100mg
$643.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment [1]:

Animal models

A modified Folts dog model

Dosage form

0.1 ~ 33 μg/(kg × min); 5 consecutive 30 min periods

Applications

AZD1283 dose-dependently increased blood flow and inhibited ADP-induced platelet aggregation with an antithrombotic ED50 value of 3 μg/(kg × min). A dose higher than 33 μg/(kg × min) was required for induction of a larger than 3.5-fold increase in bleeding time.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Bach P, Antonsson T, Bylund R, Bjrkman JA, sterlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F. Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. J Med Chem. 2013;56(17):7015-24.

Background

IC50: 0.011, 0.025 and 3.2 μM for binding, GTPγS and residual platelet count (RPC), respectively

The central role of the P2Y12 receptor in platelet function makes it an attractive target for the development of novel antiplatelet therapies. AZD1283 is found to be a potent, selective and reversible antagonist of the P2Y12 receptor.

In vitro: It was observed that the benzylic AZD1283 and its analogue 13 were both potent in the higher order residual platelet count assay in which the two tested 5-chlorothienyls showed low (IC50 >22 μM) potency [1].

In vivo: In a modified Folts model in dog, both AZD1283 and its analogue 13 could dose-dependently induce increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10.0 μg/kg/min, respectively. The dose that induced a larger than 3-fold increase in bleeding time were 33 and 100 μg/kg/min for AZD1283 and 13, respectively [2].

Clinical trials: Currenlty there is no clinical data available.

Reference:
[1] Bach P, Antonsson T, Bylund R, Björkman JA, Österlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F.   Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. J Med Chem. 2013;56(17):7015-24.

Chemical Properties

Cas No. 919351-41-0 SDF
Synonyms AZD 1283, 6-4-(Benzylsulfonyl)aminocarbonylpiperidin-1-yl-5-cyano-2-methylnicotinic acid ethyl ester
Formula C23H26N4O5S M.Wt 470.54
Solubility ≥ 18.15mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1252 mL 10.6261 mL 21.2522 mL
5 mM 0.425 mL 2.1252 mL 4.2504 mL
10 mM 0.2125 mL 1.0626 mL 2.1252 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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