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Dynapyrazole-A 2226517-75-3

Dynapyrazole-A 2226517-75-3

CAS No.: 2226517-75-3

Dynapyrazole A is a specific inhibitor of microtubule dynein that specifically inhibits the ATPase activity of microtubu
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Dynapyrazole A is a specific inhibitor of microtubule dynein that specifically inhibits the ATPase activity of microtubule-stimulated dynein but does not block the microtubule-independent basal activity.

Physicochemical Properties


Molecular Formula C20H12CLIN4O
Molecular Weight 486.69
Exact Mass 485.974
CAS # 2226517-75-3
PubChem CID 136213044
Appearance White to off-white solid powder
Density 1.9±0.1 g/cm3
Boiling Point 551.3±50.0 °C at 760 mmHg
Flash Point 287.2±30.1 °C
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.821
LogP 5.45
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 2
Heavy Atom Count 27
Complexity 668
Defined Atom Stereocenter Count 0
InChi Key VABPBCMFKJDOHP-UHFFFAOYSA-N
InChi Code

InChI=1S/C20H12ClIN4O/c21-12-3-1-11(2-4-12)20(7-8-20)17-15(10-23)18-24-19(27)14-9-13(22)5-6-16(14)26(18)25-17/h1-6,9H,7-8H2,(H,24,27)
Chemical Name

2-[1-(4-chlorophenyl)cyclopropyl]-7-iodo-5-oxo-4H-pyrazolo[1,5-a]quinazoline-3-carbonitrile
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro In MA-104 cells infected with the RVA-NMTL virus, dynapyrazole A (1–3 μg/mL, 14 h) can lower virus titers in a dose-dependent manner; its EC 50 value is 0.73 μg/mL[1].
References

[1]. Rotavirus Viroplasm Biogenesis Involves Microtubule-Based Dynein Transport Mediated by an Interaction between NSP2 and Dynein Intermediate Chain. J Virol. 2021 Oct 13;95(21):e0124621.


Solubility Data


Solubility (In Vitro) DMSO : 25 mg/mL (51.37 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0547 mL 10.2735 mL 20.5470 mL
5 mM 0.4109 mL 2.0547 mL 4.1094 mL
10 mM 0.2055 mL 1.0273 mL 2.0547 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.