93076-89-2
93076-89-2
Chemical Structure
R 59-022
Synonym(s): DKGI-I; Diacylglycerol kinase inhibitor I
- CAS No.: 93076-89-2
- Formula:C27H26FN3OS
- Molecular Weight:459.58
IUPAC Name: 6-(2-(4-((4-fluorophenyl)(phenyl)methylene)piperidin-1-yl)ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
InChIKey: MFVJXLPANKSLLD-UHFFFAOYSA-N
SMILES: O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5
Biological Activity: R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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R 59-022 | 99.82% | R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils. | ||||||||||||||||||||
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R 59-022 (Standard) | 98.09% | R 59-022 (Standard) is the analytical standard of R 59-022. This product is intended for research and analytical applications. R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils. | ||||||||||||||||||||
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Ocaperidone (Standard) | ≥98% | Ocaperidone (Standard) is the analytical standard of Ocaperidone (HY-101094). This product is intended for research and analytical applications. Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A. | ||||||||||||||||||||
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R 59-022 hydrochloride | 98.88% | R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils. | ||||||||||||||||||||
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Ritanserin | 99.68% | Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors. | ||||||||||||||||||||
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R59949 | 99.98% | R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol. | ||||||||||||||||||||
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Setoperone | Setoperone is an orally active and potent 5-HT₂ receptor antagonist and a moderate dopamine D₂ receptor blocker. Setoperone dissociates from the receptors relatively quickly, but it is easily "captured" by serotonin receptors in the body, resulting in persistent receptor inhibition even after elution. Setoperone can be used to study the negative symptoms of type II schizophrenia and associated mood disorders. | |||||||||||||||||||||
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Metrenperone | Metrenperone is an inhibitor for 5-HT2 receptor. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue. | |||||||||||||||||||||
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JNJ-3790339 | 99.65% | JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation. | ||||||||||||||||||||
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Seganserin | 99.30% | Seganserin is an orally active 5-HT receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research. | ||||||||||||||||||||
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Pirenperone | 98.97% | Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity. | ||||||||||||||||||||
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Lusaperidone | 99.81% | Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively. | ||||||||||||||||||||
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References
- [1]. de Chaffoy de Courcelles DC, et al. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. J Biol Chem. 1985 Dec 15;260(29):15762-70. [Content Brief]
- [2]. Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987 May 1;243(3):809-13. [Content Brief]
- [3]. Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenalinerelease and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990 Nov;101(3):521-6. [Content Brief]
- [4]. Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39. [Content Brief]
