Endogenous Metabolite Inhibitor

Endogenous Metabolite Inhibitors (57):

Cat. No.	Product Name	Effect	Purity

HY-13749

Sitagliptin	Inhibitor	99.75%
Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.

HY-B1232

Metyrapone	Inhibitor	99.83%
Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression.

HY-13749A

Sitagliptin phosphate	Inhibitor	99.64%
Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.

HY-106024B

Alagebrium chloride	Inhibitor	99.82%
Alagebrium chloride (ALT711) is an advanced glycation end product (AGE) inhibitor.

HY-B0251

Eplerenone	Inhibitor	99.81%
Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC₅₀ value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV).

HY-16482

Teglicar	Inhibitor	≥98.0%
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC₅₀ value of 0.68 μM and a K_i value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD).

HY-W012977

3,3-Dimethyl-1-butanol	Inhibitor	99.56%
3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).

HY-150252A

ATIC-IN-1 acetate	Inhibitor	99.96%
ATIC-IN-1 (compound 14) acetate is an inhibitor targeting to Aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC) dimerization with a K_i value of 685 nM, whcich catalyzes de novo purine biosynthesis. ATIC dimerization is crucial for its aminoimidazole carboxamide ribonucleotide (AICAR) transformylase activity. ATIC-IN-1 acetate exhibits anti-tumor activity via reduction in cell numbers and cell division rates.

HY-13749B

Sitagliptin phosphate monohydrate	Inhibitor	99.83%
Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.

HY-110036

GW-405833	Inhibitor	98.91%
GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB₂) agonist. GW405833 has EC₅₀ and K_i values of 0.65 nM and 3.92 nM for CB₂, and EC₅₀ and K_i values of 16.1 μM and 4772 nM for CB₁. GW-405833 also exhibits non-competitive CB₁ antagonist, exerting its analgesic and and anti-inflammatory effect through a CB₁ receptor (rather than CB₂) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

HY-155157

PF-07247685	Inhibitor	98.66%
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC₅₀=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice.

HY-162350

TDI-11055	Inhibitor	99.43%
TDI-11055 is an inhibitor of the epigenetic reader protein 11-19 leukemia (ENL) YEATS, which drives the oncogenic transcriptional program of acute myeloid leukemia (AML), the hematopoietic malignancy AML.

HY-137243

Adenosine 3',5'-diphosphate disodium	Inhibitor	99.12%
Adenosine 3',5'-diphosphate disodium is an hydroxysteroid sulfotransferases inhibitor.

HY-110036A

GW405833 hydrochloride	Inhibitor	99.59%
GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB₂) agonist. GW405833 has EC₅₀ and K_i values of 0.65 nM and 3.92 nM for CB₂, and EC₅₀ and K_i values of 16.1 μM and 4772 nM for CB₁. GW405833 hydrochloride also exhibits non-competitive CB₁ antagonist, exerting its analgesic effect through a CB₁ receptor (rather than CB₂) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

HY-17357

Nepafenac	Inhibitor	99.56%
Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC₅₀ of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC₅₀ = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE_₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.

HY-155156

PF-07238025	Inhibitor	99.46%
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC₅₀=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice.

HY-13749AS

Sitagliptin-d₄ phosphate	Inhibitor	99.48%
Sitagliptin-d₄ phosphate (MK-0431-d₄) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.

HY-17357S

Nepafenac-d₅	Inhibitor	98.84%
Nepafenac-d₅ (AHR-9434-d₅; AL-6515-d₅) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC₅₀ of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC₅₀ = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE_₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.

HY-137823

4-Nitrophenyl-N-acetyl-β-D-galactosaminide	Inhibitor	99.55%
4-Nitrophenyl-N-acetyl-β-D-galactosaminide has inhibitory activity against GlcNAc and GalNAc with K_is of 1.15 mM and 0.51 mM, respectively. 4-Nitrophenyl-N-acetyl-β-D-galactosaminide is extracted from Trichomonas foetus (T. foetus)

HY-B0251R

Eplerenone (Standard)	Inhibitor
Eplerenone (Standard) is the analytical standard of Eplerenone. This product is intended for research and analytical applications. Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC₅₀ value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV).

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