Maraviroc API
Appearance: White powder
Standard: in-house
Application: Lab Research
Supply Ability: 1000g per month
Purity: ≥98%
Payment: T/T, LC or DA
Delivery Time: Ready Stock in Local Warehouse, 1-3 days
Origin: China
Shipping: DHL, FedEx, TNT, EMS, By Sea, By Air
Can't sell to individuals
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Product Introduction
We supply Maraviroc
We're pleased to offer Maraviroc API, a high- quality medicinal component that's used in the treatment of HIV infection. It is produced with strict adherence to assiduity norms, icing its chastity and effectiveness. This component is available in bulk amounts and can be customized to meet specific expression conditions. Our platoon of experts works nearly with our guests to develop knitter- made results that deliver optimal results. With times of experience in the pharmaceutical assiduity, we're committed to delivering the loftiest quality products and services to our guests. communicate us moment to learn further about our Maraviroc and how it can profit your business.
What is Maraviroc API?
Maraviroc is a CCR5 antagonist that acts on MIP- 1 α, MIP- 1 β, and RANTES, with IC50 values of3.3 nM,7.2 nM, and5.2 nM in cell-free assays, independently.
it is an antiretroviral drug used to treat mortal immunodeficiency contagion( HIV) infections. It's a CCR5 antagonist that works by blocking the entry of HIV into mortal vulnerable cells. The drug is available in a tablet form and is generally specified for cases who have failed to respond to other HIV specifics or have developed resistance to them.
It is produced using advanced manufacturing processes that insure high chastity situations and thickness in every batch. It's a potent medicine with a long half- life, which means that it can be taken just formerly or doubly a day. This makes it a accessible option for cases who have difficulty clinging to complicated dosing schedules.
The drug has been considerably tested in clinical trials and has been set up to be safe and effective in reducing HIV viral cargo. still, it may not be suitable for everyone and should be taken only under the supervision of a good healthcare provider. It shouldn't be used by cases with severe liver dysfunction or those who are taking certain specifics that interact with maraviroc.
It is a important tool in the fight against HIV, and its vacuity has significantly bettered the outlook for numerous cases with the complaint. It offers a new option for cases who have exhausted other treatment options, and its accessible dosing schedule can help ameliorate adherence and overall treatment issues.
In conclusion, It is a largely effective drug that offers significant benefits for cases with HIV. It's an important tool in the ongoing battle against the complaint and has the implicit to ameliorate the lives of numerous people living with HIV.
Basic Information
Product Name: Maraviroc
CAS: 376348-65-1
MF:C29H41F2N5O
MW:513.68
EINECS:609-456-0
MDL No.:MFCD09953791
Structural formula:
Application: Lab Research
Origin: China
Delivery Time: in stock
Technical Specification
|
ITEMS |
STANDARDS |
RESULTS |
|
Appearance |
White powder |
White powder |
|
Heavy Metals |
≤10ppm |
Complies |
|
Related Substances |
Individual Impurities:≤0.5% |
0.15% |
|
Total Impurities:≤1.0% |
0.22% |
|
|
Assay (on dry basis) |
98.0%~102.0% |
101.2% |
|
Conclusion:It complies to enterprise standard. |
||
Package: 1g; 10g; or according to your demands
Storage conditions: -20 ℃, protected from light and moisture, sealed and dry
Transportation conditions: 2-8 ℃ transportation
Shelf Life:24 months
Target points
|
CCR5 |
MIP-1α |
RANTES |
MIP-1β |
|
|
3.3 nM |
5.2 nM |
7.2 nM |
In vitro research
Maraviroc API inhibits the binding of γ - S-GTP stimulated by MIP-1 β to the membrane of HEK-293 cells, indicating that it can inhibit chemokine dependent stimulation of GDP-GTP exchange on the CCR5/G protein complex. it also inhibits downstream events of chemokine induced intracellular calcium redistribution, with IC50s ranging from 7 to 30 nM when acting on MIP-1 β, MIP-1 α, and RANTES. In the same experiment, even at concentrations as high as 10 μ M, it did not trigger intracellular calcium release, indicating a lack of CCR5 stimulant activity in Maraviroc. Correspondingly, it cannot induce internalization of CCR5. it also effectively acts on HIV-1 Ba-L at low nanomolar concentrations. it inhibits all 200 pseudoviruses, with an average IC90 of 13.7 nM. When the concentration reaches 1000 times its IC50, it has no clinically significant inhibitory effect on other chemokine receptors (CCR1, 2, 3, 4, 7, 8; CXCR1, 2).
In vivo research
The half-life of Maraviroc on rats is 0.9 hours, and on dogs it is 2.3 hours. Subsequently, it was orally administered to dogs at a dose of 2 mg/kg, and after 1.5 hours, it reached Cmax (256 ng/ml) with a bioavailability of 40%. it acts on rats, with approximately 30% of the administered dose absorbed from the intestine. After adding it gel into the vagina of female RAG hu mice, HIV was injected into the vagina for 1 hour. Maraviroc gel treated mice were completely immune to HIV-1 infection, while placebo treated mice were all infected. it fully protects mice from HIV-1 infection. In the virus infected mice treated with placebo, CD4 T cells were significantly decreased, while the level was stable in the mice treated with Maraviroc gel.
Usage and Description
Research reagent widely used in molecular biology, pharmacology and other scientific research fields, strictly prohibited for use in the human body. Maraviroc is a CCR5 chemokine receptor antagonist and an antiretroviral entry inhibitor. it inhibits the entry of HIV by blocking the interaction between the viral coat protein gp120 and its receptor.
Liquid storage configuration
|
1 mg |
5 mg |
10 mg |
|
1 mM |
1.9468 mL |
9.7339 mL |
19.4678 mL |
|
5 mM |
0.3894 mL |
1.9468 mL |
3.8936 mL |
|
10 mM |
0.1947 mL |
0.9734 mL |
1.9468 mL |
|
50 mM |
0.0389 mL |
0.1947 mL |
0.3894 mL |
Classic experimental operations (for reference only)
|
Kinase experiment: |
The inhibitory effect of chemokines on CCR5 binding: Measure the binding of 125I labeled MIP-1 α, MIP-1 β, and RANTES to CCR5 using insect HEK-293 cells that stably express receptors or membranes and their products. Cells were resuspended at a density of 2 x 106 cells/ml in a binding buffer (50 mM HEPES containing 1 mM CaCl2, 5 mM MgCl2, and 0.5% bovine serum protein [BSA], pH adjusted to 7.4). In order to prepare the membrane, PBS washed cells were resuspended in a lysis buffer (20 mM HEPES, 1 mM CaCl2, 1 tablet COMPETE/50 mL, pH 7.4), then stirred in a Polygon handheld homogenizer, centrifuged at 40000 × g for 30 minutes, and then suspended in a binding buffer with a protein concentration of 0.25 mg/mL (12.5 μ g of membrane protein per well in a 96 well plate). Prepare 125I radioactive labeled MIP-1 α, MIP-1 β, and RANTES, dilute in a binding buffer, and achieve a final concentration of 400 pM. Add Maraviroc diluent to each well, with a final volume of 100 μ L. Incubate the experimental plate for 1 hour, filter through pre blocked and washed Unifilter plates, count, and dry overnight. |
|
Cell experiments: |
Cell lines: PBMC or PM-1 cells stimulated by PHA Concentrations: 0-1 μM Incubation Time: 5 or 7 days Method: Perform drug sensitivity tests on a 24 well tissue culture plate. Prepare repeated 8-point continuous dilution Maraviroc in DMSO, with a final concentration of 0.1% (vol/vol) in the experiment. PBMC or PM-1 cells infected with PHA stimulation were incubated at 37 ° C for 1 hour. Subsequently, the cells were diluted once, and 3.6 × 105 PBMC or 2.0 × 105 PM-1 cells were added to each well containing diluted Maraviroc. The experimental board was incubated at 37 ° C for 5 days (laboratory adapted strain) or 7 days (original isolated strain) in an environment containing 5% CO2 (vol/vol). All experiments contain Sakinavir (an HIV-1 protease inhibitor) and RANTES. |
|
Animal experiments: |
Animal Models: Humanized BALB/c-Rag2 −/− γ c −/− and BALB/c-Rag1 −/− γ c −/− (RAG hu) mice Formula: Dissolve in PBS, perform aseptic filtration, and then adjust the concentration to 4 mg/mL (7.8 mM). Add 3.4% hydroxyethyl cellulose (HEC) gel preparation, and obtain Maraviroc with final concentration of 5 mM in 2.2% HEC gel. Dosages: ~64 μg Administration: 25 μ L gel formula was carefully added to the vaginal vault of mice. |
Packing & Shipping
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Packing： 1kg/foil bag;5kg/carton;25kg/fiber drum; or packing as your request. Customization: l Customized logo l Customized packaging l Graphic customization
Shipping： By Courier; By Air or By Sea, according to your demands |
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Payment Term
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