AZD1981
Based on 2 publication(s) in Google Scholar
AZD1981 is the antagonist for GPR44 (also known also PTGDR2, DP2 or CRTh). AZD1981 blocks the binding of PGD2 to CRTH2. AZD1981 exhibits immunomodulatory effects and can be used in research of chronic spontaneous urticaria.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 802904-66-1
- Formula: C19H17ClN2O3S
- Molecular Weight:388.87
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AZD1981
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Biological Activity
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DP |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4.3 nM
Compound: 33
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Displacement of [3H]PGD2 from recombinant human CRTH2 expressed in HEK293 cells after 2 hrs by microbeta scintillation counting
Displacement of [3H]PGD2 from recombinant human CRTH2 expressed in HEK293 cells after 2 hrs by microbeta scintillation counting
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[PMID: 22224640] |
AZD1981 inhibits PGD2-mediated morphological changes of human eosinophils and basophils, inhibits PGD2-mediated chemotaxis of human Th2 lymphocytes and eosinophils, and blocks PGD2-mediated migration of guinea pig bone marrow eosinophils[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 802904-66-1
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Appearance Solid
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Molecular Weight 388.87
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Formula C19H17ClN2O3S
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Color White to gray
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SMILES
O=C(O)CN1C(C)=C(SC2=CC=C(Cl)C=C2)C3=C1C=CC=C3NC(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
PGD2 displays distinct effects in diffuse large B-cell lymphoma depending on different concentrations. [Abstract]2023 Feb 1;9(1):39. PMID: 36725845 -
Cell Rep
Astrocyte-derived CHI3L1 signaling impairs neurogenesis and cognition in the demyelinated hippocampus. [Abstract]2024 May 10;43(5):114226. PMID: 38733586
Solvent & Solubility
DMSO : 100 mg/mL (257.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hu S, et al., PGD2 displays distinct effects in diffuse large B-cell lymphoma depending on different concentrations. Cell Death Discov. 2023 Feb 1;9(1):39. [Content Brief]
[2]. Oliver ET, et al., Effects of an Oral CRTh2 Antagonist (AZD1981) on Eosinophil Activity and Symptoms in Chronic Spontaneous Urticaria. Int Arch Allergy Immunol. 2019;179(1):21-30. [Content Brief]
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 | 2.5716 mL | 12.8578 mL | 25.7155 mL | 64.2888 mL |
| 5 mM | 0.5143 mL | 2.5716 mL | 5.1431 mL | 12.8578 mL | |
| 10 mM | 0.2572 mL | 1.2858 mL | 2.5716 mL | 6.4289 mL | |
| 15 mM | 0.1714 mL | 0.8572 mL | 1.7144 mL | 4.2859 mL | |
| 20 mM | 0.1286 mL | 0.6429 mL | 1.2858 mL | 3.2144 mL | |
| 25 mM | 0.1029 mL | 0.5143 mL | 1.0286 mL | 2.5716 mL | |
| 30 mM | 0.0857 mL | 0.4286 mL | 0.8572 mL | 2.1430 mL | |
| 40 mM | 0.0643 mL | 0.3214 mL | 0.6429 mL | 1.6072 mL | |
| 50 mM | 0.0514 mL | 0.2572 mL | 0.5143 mL | 1.2858 mL | |
| 60 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0715 mL | |
| 80 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8036 mL | |
| 100 mM | 0.0257 mL | 0.1286 mL | 0.2572 mL | 0.6429 mL |
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