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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Cangrelor sodium (ARC69931MX; AR-C69931; Kengreal, CANREAL; Kengrexal), the tetra-sodium salt of cangrelor which is an ATP analog, is a reversible, selective and direct-acting P2Y12 inhibitor approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is distinct from the prodrug clopidogrel (Plavix) in that it is a modified ATP analog that is stable against enzymatic degradation and does not require metabolic reaction to become an active metabolite. This enables cangrelor to start working right away after infusion and allows for ongoing infusion to maintain the therapeutic effects.
| ln Vitro |
Tetrasodium Cangeler is the only effective intravenous direct potential adenosine diphosphate (ADP) P2Y12 receptor clamping agent [1]. The hP2Y12 receptor pKb of tetrasodium cangeler is 8.6-9.2 [3].
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| ln Vivo |
Cangrelor tetrasodium (10 mg/kg) not only significantly reduces BLM-induced release of inflammatory cytokines (PF4, CD40L, and MPO) but also reduces vasculature, neutrophil damage, and neutrophils in fibrotic lungs and peripheral vessels. Neutrophils damage cell aggregates and increase in BLM-treated blood [2].
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| References |
[4]. Cangrelor inhibits the binding of the active metabolites of clopidogrel and prasugrel to P2Y(12) receptors in vitro. Platelets. 2015 Aug 13:1-5. |
| Molecular Formula |
C17H21CL2F3N5NA4O12P3S2
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|---|---|
| Molecular Weight |
864.27
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| Exact Mass |
774.95
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| Elemental Analysis |
C, 23.63; H, 2.45; Cl, 8.20; F, 6.59; N, 8.10; Na, 10.64; O, 22.21; P, 10.75; S, 7.42
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| CAS # |
163706-36-3
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| Related CAS # |
Cangrelor; 163706-06-7
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| Appearance |
Solid powder
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| SMILES |
CSCCNC1=C2C(=NC(=N1)SCCC(F)(F)F)N(C=N2)[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)([O-])OP(=O)(C(P(=O)([O-])[O-])(Cl)Cl)[O-])O)O.[Na+].[Na+].[Na+].[Na+]
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| InChi Key |
COWWROCHWNGJHQ-OPKBHZIBSA-J
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| InChi Code |
InChI=1S/C17H25Cl2F3N5O12P3S2.4Na/c1-43-5-3-23-12-9-13(26-15(25-12)44-4-2-16(20,21)22)27(7-24-9)14-11(29)10(28)8(38-14)6-37-42(35,36)39-41(33,34)17(18,19)40(30,31)32;;;;/h7-8,10-11,14,28-29H,2-6H2,1H3,(H,33,34)(H,35,36)(H,23,25,26)(H2,30,31,32);;;;/q;4*+1/p-4/t8-,10-,11-,14-;;;;/m1..../s1
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| Chemical Name |
tetrasodium;[dichloro(phosphonato)methyl]-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-oxidophosphoryl]oxyphosphinate
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| Synonyms |
ARC69931; AR-C69931; AR C69931; Cangrelor; AR-C69931MX; AR C69931MX; ARC69931MX; Cangrelor tetrasodium salt
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : ~125 mg/mL (~144.63 mM)
DMSO : ~12.5 mg/mL (~14.46 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (1.45 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: 1.25 mg/mL (1.45 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: 1.25 mg/mL (1.45 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 4: 100 mg/mL (115.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1570 mL | 5.7852 mL | 11.5705 mL | |
| 5 mM | 0.2314 mL | 1.1570 mL | 2.3141 mL | |
| 10 mM | 0.1157 mL | 0.5785 mL | 1.1570 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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