Nedizantrep
Based on 1 Customer Validation
GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guinea pigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough.
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- Purity: 99.56%
- CAS No.: 2376824-99-4
- 화학식: C20H19ClN6O3
- 분자량:426.86
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
TRPA1[1].
GDC-6599 exhibits excellent TRPA1 inhibition and cross species acceptable ADME (Absorption, Distribution, Metabolism, Excretion) characteristics in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley and Wistar Han IGS rats, respectively, 8-14 weeks of age[1].
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Dosage:0-100 mg/kg
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Administration:Oral gavage (p.o.); once daily; 7 days
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Result:Extended prothrombin time (PT) and activated partial thromboplastin time (aPTT).
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Animal Model:Cynomolgus monkey[1].
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Dosage:0, 15, 50 mg/kg (male) and 30 mg/kg (female)
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Administration:Oral gavage (p.o.); once daily; 7 days
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Result:Extended coagulation parameters.
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Animal Model:Male Dunkin-Hartley guinea pigs (8 weeks old)[1].
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Dosage:0-3 mg/kg
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Administration:Oral gavage (p.o.); were dosed 75 min prior to imaging
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Result:Inhibited blood perfusion, prolonged perfusion time, and reduced maximum perfusion level.
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Animal Model:Cinnamaldehyde induced cough model in guinea pigs[1].
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Dosage:0-3 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Reduced the frequency of coughing.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2376824-99-4
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Appearance Solid
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분자량 426.86
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화학식 C20H19ClN6O3
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Color White to light yellow
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SMILES
O=C1C2=C(N=CN2C)N=C(N1CC3=NC([C@H]4C[C@H](C5=CC=C(C=C5)Cl)OC4)=NO3)C
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Synonyms
GDC-6599
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (234.27 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, 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.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.86 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.86 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 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.
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.
순도&문서
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Terrett JA, et al. Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease. J Med Chem. 2024 Mar 14;67(5):3287-3306. doi: 10.1021/acs.jmedchem.3c02121. Epub 2024 Mar 3. PMID: 38431835. [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, 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 | 2.3427 mL | 11.7134 mL | 23.4269 mL | 58.5672 mL |
| 5 mM | 0.4685 mL | 2.3427 mL | 4.6854 mL | 11.7134 mL | |
| 10 mM | 0.2343 mL | 1.1713 mL | 2.3427 mL | 5.8567 mL | |
| 15 mM | 0.1562 mL | 0.7809 mL | 1.5618 mL | 3.9045 mL | |
| 20 mM | 0.1171 mL | 0.5857 mL | 1.1713 mL | 2.9284 mL | |
| 25 mM | 0.0937 mL | 0.4685 mL | 0.9371 mL | 2.3427 mL | |
| 30 mM | 0.0781 mL | 0.3904 mL | 0.7809 mL | 1.9522 mL | |
| 40 mM | 0.0586 mL | 0.2928 mL | 0.5857 mL | 1.4642 mL | |
| 50 mM | 0.0469 mL | 0.2343 mL | 0.4685 mL | 1.1713 mL | |
| 60 mM | 0.0390 mL | 0.1952 mL | 0.3904 mL | 0.9761 mL | |
| 80 mM | 0.0293 mL | 0.1464 mL | 0.2928 mL | 0.7321 mL | |
| 100 mM | 0.0234 mL | 0.1171 mL | 0.2343 mL | 0.5857 mL |
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