| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
Vermicolpan is an orally bioavailable inhibitor of complement factor D (FD; CFD). Complement factor D is a serine protease that cleaves complement factor B and possesses potential complement system inhibitory activity. Upon administration, Vermicolpan targets and blocks the activity of FD, thereby inhibiting the cleavage of complement factor B into complement factor Bα and complement factor β in the alternative complement cascade pathway. This inhibits FD-mediated signaling and activation of the alternative complement pathway (ACP), blocking complement-mediated hemolysis in paroxysmal nocturnal hemoglobinuria (PNH) and preventing ACP-induced tissue damage. FD plays a crucial role in ACP activation.
|
| Molecular Formula |
C29H28BRN7O3
|
|---|---|
| Molecular Weight |
602.4817
|
| Exact Mass |
601.143
|
| CAS # |
2086178-00-7
|
| PubChem CID |
126642840
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.1
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
40
|
| Complexity |
1010
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
BrC1C([H])=C([H])C(C([H])([H])[H])=C(N=1)N([H])C([C@]1([H])C([H])([H])[C@@]2(C([H])([H])[H])C([H])([H])[C@@]2([H])N1C(C([H])([H])N1C2C([H])=C([H])C(C3=C([H])N=C(C([H])([H])[H])N=C3[H])=C([H])C=2C(C(C([H])([H])[H])=O)=N1)=O)=O
|
| InChi Key |
OCXAGXCMZACNEC-CTWZREHQSA-N
|
| InChi Code |
InChI=1S/C29H28BrN7O3/c1-15-5-8-24(30)33-27(15)34-28(40)22-10-29(4)11-23(29)37(22)25(39)14-36-21-7-6-18(19-12-31-17(3)32-13-19)9-20(21)26(35-36)16(2)38/h5-9,12-13,22-23H,10-11,14H2,1-4H3,(H,33,34,40)/t22-,23+,29-/m0/s1
|
| Chemical Name |
(1R,3S,5R)-2-[2-[3-acetyl-5-(2-methylpyrimidin-5-yl)indazol-1-yl]acetyl]-N-(6-bromo-3-methylpyridin-2-yl)-5-methyl-2-azabicyclo[3.1.0]hexane-3-carboxamide
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO: 50 mg/mL (82.99 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.66 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.66 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 10.0 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: ≥ 1 mg/mL (1.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6598 mL | 8.2990 mL | 16.5981 mL | |
| 5 mM | 0.3320 mL | 1.6598 mL | 3.3196 mL | |
| 10 mM | 0.1660 mL | 0.8299 mL | 1.6598 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05097989
Conditions:Lupus Nephritis|Immunoglobulin A Nephropathy|IgAN|LNLink: https://clinicaltrials.gov/ct2/show/NCT06071442
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT05259085
Conditions:Impaired Hepatic Function|Healthy
Title:Study of ALXN2050 in Adult Participants With Generalized Myasthenia Gravis
Status:Terminated
updateDate:2025-01-09
Ctid:NCT05218096
Link: https://clinicaltrials.gov/ct2/show/NCT05218096
Conditions:Generalized Myasthenia Gravis|Myasthenia GravisLink: https://clinicaltrials.gov/ct2/show/NCT04170023
Conditions:Paroxysmal Nocturnal Hemoglobinuria (PNH)Link: https://clinicaltrials.gov/ct2/show/NCT04623710
Conditions:Renal Impairment|HealthyLink: https://clinicaltrials.gov/ct2/show/NCT05202145
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04952545
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04933682
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04660890
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT05047458
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT05047484
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04709081
Conditions:HealthyProducts are for research use only; We do not sell to patients
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