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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Galidesivir HCl (formerly known as BCX-4430 hydrochloride; Immucillin-A) is an antiviral drug and an adenosine analogue. Galidesivir was originally intended as a treatment for Hepatitis C, but subsequently developed as a potential treatment for deadly filovirus infections such as Ebola virus disease and Marburg virus disease. Galidesivir also shows broad-spectrum antiviral effectiveness against a range of other RNA virus families, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses and flaviviruses. BCX4430 has been demonstrated to protect against both Ebola and Marburg viruses in both rodents and monkeys, even when administered up to 48 hours after infection.
| ln Vitro |
Viral RNA polymerase incorporates the drug's monophosphate molecule into the expanding RNA chain, resulting in premature chain termination. Cell division phosphorylates Galidesivir (BCX4430) hydrochloride to a triphosphate that resembles ATP [1]. YFV infection of Vero cells is efficiently inhibited by hydrochloric acid. According to the neutral red food assay, the EC50 is 8.3 μg/mL (24.5 μM) [3].
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| ln Vivo |
Hydrochloride galidesivir (BCX4430) administered intramuscularly, intraperitoneally, orally, is effective against a range of experimental infections. In nonclinical tests including deadly infections with the Ebola, Marburg, Rift Valley disease, and yellow fever viruses, galidevir hydrochloride has demonstrated a notable level of efficacy [1]. In a hamster model of yellow fever (YF), galidevir hydrochloride (4 mg/kg; intraperitoneal injection; twice daily for 7 days) is efficacious [4].
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| Animal Protocol |
Animal/Disease Models: Female Syrian golden hamsters (hamsters infected with YF virus)[4]
Doses: 4 mg/kg of body weight Route of Administration: Ip; twice a day for 7 days Experimental Results: Dramatically improved the survival rate of hamsters infected with YFV . |
| References |
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| Additional Infomation |
Galidesivir Hydrochloride is the hydrochloride salt form of galidesivir, an adenosine analog and RNA polymerase inhibitor, with potential broad-spectrum antiviral activity. Upon administration, galidesivir is metabolized to its monophosphate form, which is then converted into the active triphosphate nucleotide. Galidesivir triphosphate binds to viral RNA-dependent RNA polymerase (RdRp) and gets incorporated into the growing viral RNA strand, which leads to premature chain termination. This prevents viral transcription and replication.
See also: Galidesivir (annotation moved to). |
| Molecular Formula |
C11H15N5O3.HCL
|
|---|---|
| Molecular Weight |
301.72944
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| Exact Mass |
301.094
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| CAS # |
222631-44-9
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| Related CAS # |
Galidesivir;249503-25-1
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| PubChem CID |
69211190
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
20
|
| Complexity |
334
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
O[C@H]1[C@H](C2=CNC3=C2N=CN=C3N)N[C@H](CO)[C@H]1O.Cl
|
| InChi Key |
PCCHVYNGFMEGIG-QPAIBFMUSA-N
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| InChi Code |
InChI=1S/C11H15N5O3.ClH/c12-11-8-6(14-3-15-11)4(1-13-8)7-10(19)9(18)5(2-17)16-7/h1,3,5,7,9-10,13,16-19H,2H2,(H2,12,14,15)1H/t5-,7+,9-,10+/m1./s1
|
| Chemical Name |
(2S,3S,4R,5R)-2-(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)pyrrolidine-3,4-diol hydrochloride
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| Synonyms |
BCX4430 BCX 4430 BCX-4430. Immucillin-A.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~105 mg/mL (~347.99 mM)
H2O : ≥ 41 mg/mL (~135.88 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.25 mg/mL (17.40 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 52.5 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: ≥ 5.25 mg/mL (17.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 52.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (331.42 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3142 mL | 16.5711 mL | 33.1422 mL | |
| 5 mM | 0.6628 mL | 3.3142 mL | 6.6284 mL | |
| 10 mM | 0.3314 mL | 1.6571 mL | 3.3142 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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