| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
With an IC50 of 900 nM, PFV IN with the S217H alteration is ten times less sensitive to raltegravir. S217Q PFV IN is equally sensitive to Raltegravir as the WT enzyme[1], while PFV IN exhibits 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, demonstrating a roughly twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. Raltegravir is not metabolized hepatically, but rather via glucuronidation. In human T lymphoid cell cultures, raltegravir exhibits strong in vitro action against HIV-1, with a 95% inhibitory concentration of 31±20 nM. When raltegravir is evaluated in CEMx174 cells, it also exhibits activity against HIV-2, with an IC95 of 6 nM. The main metabolic pathway for raltegravir is glucuronidation. It is not advisable to use medications that strongly activate the glucuronidation enzyme UGT1A1, as they drastically lower Raltegravir concentrations. Raltegravir has minimal effects on the activity of hepatic cytochrome P450. Neither CYP3A4-dependent testosterone 6-β-hydroxylase activity nor CYP3A4 RNA expression are induced by raltegravir[2]. The cellular permeeativity of raltegravir is decreased when magnesium and calcium are present [3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs) effectively prevent viral replication[4]. Raltegravir effectively inhibits SIVmac251 replication in acutely infected human lymphoid CD4+ T-cell lines MT -4 and CEMx174, with an EC90 in the low nanomolar range[5].
|
|---|---|
| ln Vivo |
Rateltelevir improves the viro-immunological status of nonhuman primates infected with SIVmac251 as it progresses. Raltegravir monotherapy results in an undetectable viral load in one non-human primate[5].
|
| References |
| Molecular Formula |
C20H22FN6NAO5
|
|---|---|
| Molecular Weight |
468.414058208466
|
| Exact Mass |
466.137
|
| CAS # |
1292804-07-9
|
| Related CAS # |
Raltegravir;518048-05-0;Raltegravir potassium;871038-72-1
|
| PubChem CID |
44569174
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
33
|
| Complexity |
843
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
QLBNDXLKPYXCIW-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C20H21FN6O5.Na/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11;/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30);/q;+1/p-1
|
| Chemical Name |
sodium;4-[(4-fluorophenyl)methylcarbamoyl]-1-methyl-2-[2-[(5-methyl-1,3,4-oxadiazole-2-carbonyl)amino]propan-2-yl]-6-oxopyrimidin-5-olate
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1349 mL | 10.6744 mL | 21.3488 mL | |
| 5 mM | 0.4270 mL | 2.1349 mL | 4.2698 mL | |
| 10 mM | 0.2135 mL | 1.0674 mL | 2.1349 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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