Metabolism Standards

Trilaciclib (hydrochloride) (Standard) is the analytical standard of Trilaciclib (hydrochloride). This product is intended for research and analytical applications. Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC₅₀s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

Gestrinone (Standard) is the analytical standard of Gestrinone. This product is intended for research and analytical applications. Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC₅₀ of 43.67 μM. Gestrinone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Asenapine (Standard) is the analytical standard of Asenapine. This product is intended for research and analytical applications. Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.

Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (K_i=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.

Sarizotan (Standard) is the analytical standard of Sarizotan. This product is intended for research and analytical applications. Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively.

Pipamperone (Standard) is the analytical standard of Pipamperone (HY-100703). This product is intended for research and analytical applications. Pipamperone (Floropipamide) is a butyrophenone derivative and high-affinity antagonist of 5-HT_2A receptor (pK_i=8.2) and D₄ receptor (pK_i=8.0). Pipamperone is also a low-affinity antagonist of D₂ receptor (pK_i=6.7). Pipamperone affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease.

Treprostinil (Standard) is the analytical standard of Treprostinil. This product is intended for research and analytical applications. Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC₅₀ values of 0.6±0.1 and 6.2±1.2 nM, respectively.

Trifarotene (Standard) is the analytical standard of Trifarotene. This product is intended for research and analytical applications. Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC₅₀=7.7 nM) over RARα (EC₅₀=500 nM) and RARβ (EC₅₀=125 nM), respectively.

Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.

Vonoprazan (Standard) is the analytical standard of Vonoprazan. This product is intended for research and analytical applications. Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H⁺,K⁺-ATPase activity in porcine gastric microsomes with an IC₅₀ of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori.

4-Hydroxymephenytoin (Standard) is the analytical standard of 4-Hydroxymephenytoin. This product is intended for research and analytical applications. 4-Hydroxymephenytoin is a metabolism of an antiepileptic agent mephenytoin, which is used as a CYP2C19 substrate.

RPR121056 (Standard) is the analytical standard of RPR121056. This product is intended for research and analytical applications. RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1].

HQNO (Standard) is the analytical standard of HQNO. This product is intended for research and analytical applications. HQNO, secreted by P. aeruginosa, is a potent electron transport chain inhibitor with a Kd of 64 nM for complex III[1]. HQNO is a potent inhibitor of mitochondrial NDH-2 in many species[2].

Diethyl phthalate (Standard) is the analytical standard of Diethyl phthalate. This product is intended for research and analytical applications. Diethyl phthalate is an endocrine disruptor that has the activity of affecting the apoptosis system of PC12 cells. Diethyl phthalate is widely used in a variety of plastics and personal care products. Diethyl phthalate has shown the potential to induce male reproductive toxicity unrelated to androgens in animal experiments.