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MedKoo Cat#: 558179 | Name: Pamicogrel
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pamicogrel is a cyclooxygenase inhibitor with platelet anti-aggregatory properties which is under development by Kanebo for chronic arterial occlusion. Pamicogrel also has potential in both prophylaxis and treatment of ischemic brain injury.

Chemical Structure

Pamicogrel
Pamicogrel
CAS#101001-34-7

Theoretical Analysis

MedKoo Cat#: 558179

Name: Pamicogrel

CAS#: 101001-34-7

Chemical Formula: C25H24N2O4S

Exact Mass: 448.1457

Molecular Weight: 448.54

Elemental Analysis: C, 66.95; H, 5.39; N, 6.25; O, 14.27; S, 7.15

Price and Availability

Size Price Availability Quantity
5mg USD 210.00 2 Weeks
25mg USD 400.00 2 Weeks
100mg USD 830.00 2 Weeks
250mg USD 1,450.00 2 Weeks
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Related CAS #
No Data
Synonym
Pamicogrel; KBT-3022; KBT3022; KBT 3022;
IUPAC/Chemical Name
1H-Pyrrole-1-acetic acid, 2-(4,5-bis(4-methoxyphenyl)-2-thiazolyl)-, ethyl ester
InChi Key
ISCHOARKJADAKJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H24N2O4S/c1-4-31-22(28)16-27-15-5-6-21(27)25-26-23(17-7-11-19(29-2)12-8-17)24(32-25)18-9-13-20(30-3)14-10-18/h5-15H,4,16H2,1-3H3
SMILES Code
O=C(OCC)CN1C(C2=NC(C3=CC=C(OC)C=C3)=C(C4=CC=C(OC)C=C4)S2)=CC=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Pamicogrel (KBT3022) is a cyclooxygenase (COX) inhibitor.
In vitro activity:
KBT-3022 and desethyl KBT-3022 inhibited cyclooxygenase from ovine seminal gland with IC50 values of 0.69 and 0.43 microM, respectively. At concentrations higher than those required for cyclooxygenase inhibition, desethyl KBT-3022 inhibited cAMP-phosphodiesterase, specific binding of U46619, and release of phosphatidic acid from thrombin-stimulated platelets. Reference: Gen Pharmacol. 1997 Feb;28(2):229-35. https://pubmed.ncbi.nlm.nih.gov/9013200/
In vivo activity:
The antithrombotic effect of desethyl KBT-3022, which is the main active metabolite of the new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl] pyrrol-1-ylacetate; a cyclooxygenase inhibitor), was determined using a photochemically induced arterial thrombosis model in the rat femoral artery. Pretreatment with desethyl KBT-3022 (0.1, 0.3 and 1 mg/kg, i.v.) prolonged the time required to achieve thrombotic occlusion in the femoral artery and inhibited collagen-induced platelet aggregation in whole blood ex vivo, each in a dose-dependent manner. In all 6 rats used, particularly at the highest dose (1 mg/kg, i.v.) tested, cyclic variations in blood flow were hardly ever observed and complete cessation of blood flow did not occur during the 30-min observation time. Reference: Eur J Pharmacol. 1997 Jun 11;328(2-3):183-9. https://pubmed.ncbi.nlm.nih.gov/9218700/
Solvent mg/mL mM
Solubility
DMF 10.0 22.00
DMF:PBS (pH 7.2) (1:1) 0.5 1.10
DMSO 5.0 11.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 448.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Matsuo K, Yokota K, Yamashita A, Oda M. The mechanism of action of KBT-3022, a new antiplatelet agent. Gen Pharmacol. 1997 Feb;28(2):229-35. doi: 10.1016/s0306-3623(96)00190-5. PMID: 9013200. 2. Yokota K, Yamamoto N, Obata Y, Oda M. Inhibitory effects of the new anti-platelet agent KBT-3022 and its metabolite on rabbit neutrophil function in vitro. Jpn J Pharmacol. 1996 Apr;70(4):291-302. doi: 10.1254/jjp.70.291. Erratum in: Jpn J Pharmacol 1997 Feb;73(2):183. PMID: 8847836. 1. Matsuo K, Yokota K, Yamashita A, Oda M. The mechanism of action of KBT-3022, a new antiplatelet agent. Gen Pharmacol. 1997 Feb;28(2):229-35. doi: 10.1016/s0306-3623(96)00190-5. PMID: 9013200. 2. Yokota K, Yamamoto N, Obata Y, Oda M. Inhibitory effects of the new anti-platelet agent KBT-3022 and its metabolite on rabbit neutrophil function in vitro. Jpn J Pharmacol. 1996 Apr;70(4):291-302. doi: 10.1254/jjp.70.291. Erratum in: Jpn J Pharmacol 1997 Feb;73(2):183. PMID: 8847836. 3. Shimazawa M, Takiguchi Y, Umemura K, Kondo K, Nakashima M. Antithrombotic effects in a rat model of aspirin-insensitive arterial thrombosis of desethyl KBT-3022, the main active metabolite of a new antiplatelet agent, KBT-3022. Eur J Pharmacol. 1997 Jun 11;328(2-3):183-9. doi: 10.1016/s0014-2999(97)83044-0. PMID: 9218700. 4. Yamamoto N, Yokota K, Yamashita A, Oda M. Effect of KBT-3022, a new cyclooxygenase inhibitor, on experimental brain edema in vitro and in vivo. Eur J Pharmacol. 1996 Feb 22;297(3):225-31. doi: 10.1016/0014-2999(95)00777-6. PMID: 8666054.
In vitro protocol:
1. Matsuo K, Yokota K, Yamashita A, Oda M. The mechanism of action of KBT-3022, a new antiplatelet agent. Gen Pharmacol. 1997 Feb;28(2):229-35. doi: 10.1016/s0306-3623(96)00190-5. PMID: 9013200. 2. Yokota K, Yamamoto N, Obata Y, Oda M. Inhibitory effects of the new anti-platelet agent KBT-3022 and its metabolite on rabbit neutrophil function in vitro. Jpn J Pharmacol. 1996 Apr;70(4):291-302. doi: 10.1254/jjp.70.291. Erratum in: Jpn J Pharmacol 1997 Feb;73(2):183. PMID: 8847836.
In vivo protocol:
1. Shimazawa M, Takiguchi Y, Umemura K, Kondo K, Nakashima M. Antithrombotic effects in a rat model of aspirin-insensitive arterial thrombosis of desethyl KBT-3022, the main active metabolite of a new antiplatelet agent, KBT-3022. Eur J Pharmacol. 1997 Jun 11;328(2-3):183-9. doi: 10.1016/s0014-2999(97)83044-0. PMID: 9218700. 2. Yamamoto N, Yokota K, Yamashita A, Oda M. Effect of KBT-3022, a new cyclooxygenase inhibitor, on experimental brain edema in vitro and in vivo. Eur J Pharmacol. 1996 Feb 22;297(3):225-31. doi: 10.1016/0014-2999(95)00777-6. PMID: 8666054.
1: Light P. Pamicogrel (Kanebo). IDrugs. 1999 Sep;2(9):938-42. PubMed PMID:16121308. 2: Tanemoto, K. (2001). Pamicogrel inhibits platelet aggregation. Inpharma, 1272, 27.

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