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Results for "

antagonistic activity

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (212) Cardiovascular Disease (80) Endocrinology (85) Infection (54) Inflammation/Immunology (146) Metabolic Disease (53) Neurological Disease (258)
Click Chemistry:	Alkynes (1)

626

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

(RS)-CPP (±)-CPP	iGluR	Neurological Disease
(RS)-CPP ((±)-CPP) is a potent and selective NMDA antagonist. (RS)-CPP inhibits central neuron responses, and has anticonvulsant activity .

SDZ NKT 343	Neurokinin Receptor	Neurological Disease
SDZ NKT 343 is a selective, orally active NK₁ receptor antagonist with an IC₅₀ of 0.62 nM against human NK₁ receptor. SDZ NKT 343 has good analgesic activity .

SB-209247	Leukotriene Receptor	Inflammation/Immunology
SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a K_i of 0.78 nM. SB-209247 blocks LTB4-induced Ca ²⁺ mobilization with an IC₅₀ of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity .

SM-2470	Adrenergic Receptor	Neurological Disease Metabolic Disease
SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats . SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization .

σ1 Receptor/μ Opioid receptor modulator 1	Sigma Receptor Opioid Receptor	Neurological Disease
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with K_is of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .

GABAA receptor agent 6	GABA Receptor	Neurological Disease
GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an K_i of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

GLI antagonist-1	Gli	Cancer
GLI antagonist-1 is a potent GLI antagonist with an IC₅₀ value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .

CXCR4 antagonist 1	CXCR HIV	Infection
CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity .

Estrogen receptor antagonist 7	Estrogen Receptor/ERR	Cancer
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .

SF-1 antagonist-1	Others	Cancer
SF-1 antagonist-1 (compound 11) is a antagonist of steroidogenic factor 1 (SF-1). SF-1 antagonist-1 affects SF-1 transcriptional activity with an EC₅₀ value of ＜200 nM. SF-1 antagonist-1 inhibits the proliferation of Rat Leydig tumor cells. SF-1 antagonist-1 can be used for the research of cancer .

GluN2B-NMDAR antagonist-1	iGluR	Neurological Disease Inflammation/Immunology
GluN2B-NMDAR antagonist-1 is an orally active GluN2B-NMDAR antagonist. GluN2B-NMDAR antagonist-1 has neuroprotective activity. GluN2B-NMDAR antagonist-1 can be used for research of ischemic injury .

Androgen receptor antagonist 4	Androgen Receptor	Cancer
Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC₅₀ of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .

Androgen receptor antagonist 3	Androgen Receptor	Cancer
Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC₅₀ of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities .

GPR183 antagonist-3	EBI2/GPR183	Inflammation/Immunology
GPR183 antagonist-3 (compound 33) is an oral active GPR183 antagonist with the IC₅₀ of 8.7 μM. GPR183 antagonist-3 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, and improves the pathological symptoms of DSS-induced experimental colitis .

TRPV3 antagonist 74a	TRP Channel	Neurological Disease
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain .

RXR antagonist 1	RAR/RXR	Neurological Disease Metabolic Disease Cancer
RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA₂ of 8.06. RXR antagonist 1 can be used for type 2 diabetes research .

EP4 receptor antagonist 2	Prostaglandin Receptor	Cancer
EP4 receptor antagonist 2 (compound 2-13) is a potent EP4 receptor antagonist with an IC₅₀ of 7.8 nM. EP4 receptor antagonist 2 shows antitumor activity .

CCR5 antagonist 2	CCR HIV	Infection
CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC₅₀ of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities .

CCR5 antagonist 3	CCR HIV	Infection
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC₅₀ of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities .

LTB4 antagonist 3	Leukotriene Receptor	Inflammation/Immunology
LTB4 antagonist 3 (compound 24e) is a leukotriene B4 (LTB4) antagonist with an IC₅₀ value of 477 nM. LTB4 antagonist 3 has anti-inflammatory activity .

Androgen receptor antagonist 5	Androgen Receptor	Cancer
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC₅₀ value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .

Ecastolol	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.

TMBIM6 antagonist-1	mTOR	Cancer
TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca ²⁺ .

LTB4 antagonist 2	Leukotriene Receptor	Inflammation/Immunology
LTB4 antagonist 2, a carboxamide-acid compound, is an antagonist of leukotriene B4 (LTB4) with potentially anti-inflammatory activity. LTB4 antagonist 2 shows good affinity for the LTB4 receptor with IC₅₀ of 439 nM .

PAR4 antagonist 5	Protease Activated Receptor (PAR)	Cardiovascular Disease
PAR4 antagonist 5 (compound 1) is a PAR4 antagonist with an IC₅₀ less than 20 μM and potent anti-platelet aggregation activity. PAR4 antagonist 5 can be used for research of thrombosis disease .

Elucaine	mAChR	Inflammation/Immunology
Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.

CCX354 1 Publications Verification	CCR	Inflammation/Immunology Endocrinology
CCX354 is an antagonist of CCR1, with anti-inflammatory activity.

Hexamethonium Bromide 2 Publications Verification	nAChR Apoptosis	Cardiovascular Disease Neurological Disease
Hexamethonium Bromide is a non-selective ganglionic *nicotinic-receptor antagonist* (nAChR)** antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .

AR antagonist 6	Androgen Receptor	Endocrinology
AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model. .

5-HT2 antagonist 1	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.

RAGE antagonist peptide 2 Publications Verification	Amyloid-β	Inflammation/Immunology Cancer
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities .

Adenosine receptor antagonist 2	Adenosine Receptor	Cancer
Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC₅₀s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity .

GRPR antagonist-2	Others	Cancer
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC₅₀ of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity .

NOD1 antagonist-1	NOD-like Receptor (NLR)	Inflammation/Immunology
NOD1 antagonist-1 (compound 37) exhibits an antagonistic activity towards NOD1 and a weak NOD1/NOD2 selectivity, with IC₅₀s of 9.18 μM and 20.8 μM, respectively .

Pamatolol	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Pamatolol is a cardioselective beta-adrenoceptor antagonist without sympathomimetic activity.

CCK-B Receptor Antagonist 2	Cholecystokinin Receptor	Metabolic Disease
CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC₅₀ value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC₅₀ of 1.82 μM .

Aschantin	mTOR Cytochrome P450	Infection Cardiovascular Disease Cancer
Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca ²⁺-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .

CRTh2 antagonist 3	Prostaglandin Receptor PDK-1	Cardiovascular Disease Inflammation/Immunology
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist . CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC₅₀ of 2 μM and a K_d of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation .

RAGE antagonist peptide TFA 2 Publications Verification	Amyloid-β	Inflammation/Immunology Cancer
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities .

GnRH-R antagonist 1	GnRH Receptor	Cancer
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC₅₀=0.57 nM) and potent in vitro antagonistic activity (IC₅₀=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing .

Sulamserod RS-100302	5-HT Receptor	Cardiovascular Disease
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.

SC-52012	Others	Cardiovascular Disease
HY-19163 is an orally active fibrinogen receptor antagonist, with antiplatelet activities.

UNBS5162 5+ Cited Publications	CXCR Autophagy	Endocrinology Cancer
UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

GPR132 antagonist 1	Others	Metabolic Disease
GPR132 antagonist 1 (GPR132-B-160, Compound 25) is a GPR132 antagonist with an EC₅₀ value of 0.075 μM. GPR132 antagonist 1 has promote insulin secretion activity with an EC₅₀ value of 0.7 μM .

GRPR antagonist-1	Others	Cancer
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC₅₀ of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity .

Androgen receptor antagonist 7	Androgen Receptor	Cancer
Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC₅₀ value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI₅₀ value of 7.9 µM .

Cat. No.	Product Name

HY-L070

Neuroprotective Compound Library

1,068 compounds

Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases.

MCE offers a unique collection of 1,068 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

HY-L145

Antihypertensive Compound Library

487 compounds

The majority of hypertensive patients have primary (or essential) hypertension, that is, hypertension in which secondary causes are not present. Management aims to control arterial pressure, prevent end-organ damage (cerebrovascular, cardiovascular, and renal), and reduce the risk of premature death.

Antihypertensive drugs may be divided into two broad groups, the first group being those which directly or indirectly block the renin–angiotensin system (RAS), for example, ACEIs, angiotensin receptor antagonists (ARAs), direct renin inhibitors (DRIs), and to a lesser extent β-blockers. The second group of drugs works by increasing water and sodium excretion, thereby reducing intravascular volume, or by causing vasodilatation through non-RAS pathways, for example, diuretics and calcium channel blockers (CCBs).

MCE offers a unique collection of 487 compounds with identified and potential antihypertensive activity. MCE Antihypertensive Compound Library is critical for antihypertensive drug discovery and development.

Cat. No.	Product Name	Target	Research Area

HY-P2276A

Pep2-8 TFA

Peptides Others

Pep2-8 is a peptide which has enhanced the antagonistic activity of proprotein convertase subtilin/ kexin 9 type (PCSK9) .

HY-P2268

RAGE antagonist peptide 2 Publications Verification	Amyloid-β	Inflammation/Immunology Cancer
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities .

HY-P2268A

RAGE antagonist peptide TFA 2 Publications Verification	Amyloid-β	Inflammation/Immunology Cancer
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities .

HY-B0686

Eptifibatide 5+ Cited Publications	Integrin	Cardiovascular Disease
Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity .

HY-144285

CXCR4 antagonist 4	CXCR HIV	Inflammation/Immunology
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC₅₀=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC₅₀=7 nM) .

HY-B0686A

Eptifibatide monoacetate	Integrin	Cardiovascular Disease
Eptifibatide monoacetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity .

HY-P1869

Neuropeptide EI, rat	MCHR1 (GPR24) Melanocortin Receptor	Neurological Disease Endocrinology
Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms .

HY-P1750

Shepherdin (79-87)	HSP Survivin	Cancer
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .

HY-P1750A

Shepherdin (79-87) (TFA)	HSP Survivin	Cancer
Shepherdin (79-87) TFA is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .

HY-P2355A

{Boc}-Phe-Leu-Phe-Leu-Phe TFA	Formyl Peptide Receptor (FPR)	Inflammation/Immunology
{Boc}-Phe-Leu-Phe-Leu-Phe TFA is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .

HY-P1104A

FC131 TFA

CXCR HIV Infection

FC131 TFA is a CXCR4 antagonist, inhibits [ ¹²⁵I]-SDF-1 binding to CXCR4, with an IC₅₀ of 4.5 nM. Anti-HIV activity .

HY-P2355

{Boc}-Phe-Leu-Phe-Leu-Phe	Formyl Peptide Receptor (FPR)	Inflammation/Immunology
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .

HY-P1415

Norleual	c-Met/HGFR Angiotensin Receptor	Neurological Disease Metabolic Disease
Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC₅₀ of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .

HY-P1795

N-Boc-Phe-Leu-Phe-Leu-Phe 1 Publications Verification Boc-FLFLF	Formyl Peptide Receptor (FPR)	Neurological Disease
N-Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) is a formyl peptide receptor 1 (FPR1) antagonist, which increases pain effects and inhibits antinociceptive activity of annexin .

HY-P1167

[Orn5]-URP	Urotensin Receptor	Cardiovascular Disease
[Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP displays no agonist activity .

HY-P1415A

Norleual TFA 1 Publications Verification	c-Met/HGFR Angiotensin Receptor	Neurological Disease Metabolic Disease
Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC₅₀ of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .

HY-P1104

FC131

CXCR HIV Infection

FC131 is a potent CXCR4 antagonist. FC131 inhibits [ ¹²⁵I]-SDF-1 binding to CXCR4 with an IC₅₀ of 4.5 nM. FC131 has anti-HIV activity .

HY-P4874

ACTH (7-38) (human)	Melanocortin Receptor	Metabolic Disease
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .

HY-P1167A

[Orn5]-URP TFA	Urotensin Receptor	Cardiovascular Disease
[Orn5]-URP TFA is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP TFA displays no agonist activity .

HY-P1102

TC14012 2 Publications Verification	CXCR HIV	Infection Cancer
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .

HY-P1285

Conantokin R Con-R	iGluR	Neurological Disease
Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC₅₀ of 93 nM. Conantokin R binds Zn ²⁺ and Mg ²⁺ with K_ds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity .

HY-P1329

CTOP	Opioid Receptor	Neurological Disease
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .

HY-P1102A

TC14012 TFA	CXCR HIV	Infection Cancer
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC₅₀ of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC₅₀ of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .

HY-P1329A

CTOP TFA 1 Publications Verification	Opioid Receptor	Neurological Disease
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .

HY-106268A

Larazotide acetate 3 Publications Verification	Gap Junction Protein	Inflammation/Immunology
Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC₅₀s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide acetate can be used for the research of celiac disease and infection.

HY-P3664

[D-Phe2,D-Ala6]-LH-RH

Wy 18185
GnRH Receptor Endocrinology

[D-Phe2,D-Ala6]-LH-RH is a potent LH-RH antagonist. [D-Phe2,D-Ala6]-LH-RH shows anti-LH/FSH-RH and antiovulatory activities .

HY-106268

Larazotide	Gap Junction Protein	Infection Inflammation/Immunology
Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC₅₀s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection .

HY-P1651

SOR-C13	TRP Channel	Cancer
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC₅₀ value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .

HY-P1651A

SOR-C13 TFA	TRP Channel	Cancer
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC₅₀ value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .

HY-P1159

[D-p-Cl-Phe6,Leu17]-VIP	Peptides	Neurological Disease Inflammation/Immunology
[D-p-Cl-Phe6,Leu17]-VIP is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC₅₀ of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP has no activity on glucagon, secretin or GRF receptors .

HY-P0205A

Saralasin acetate hydrate [Sar1,Ala8] Angiotensin II acetate hydrate	Angiotensin Receptor	Cardiovascular Disease Inflammation/Immunology
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a K_i value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .

HY-P0205

Saralasin [Sar1,Ala8] Angiotensin II	Angiotensin Receptor	Cardiovascular Disease Inflammation/Immunology
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a K_i value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .

HY-P1722

Spantide II	Neurokinin Receptor	Inflammation/Immunology
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis .

HY-P0205B

Saralasin TFA [Sar1,Ala8] Angiotensin II TFA	Angiotensin Receptor	Cardiovascular Disease Inflammation/Immunology
Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a K_i value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .

HY-P1159A

[D-p-Cl-Phe6,Leu17]-VIP TFA	Peptides	Neurological Disease Inflammation/Immunology
[D-p-Cl-Phe6,Leu17]-VIP TFA is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC₅₀ of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP TFA has no activity on glucagon, secretin or GRF receptors .

HY-P1812

AUNP-12 NP-12	PD-1/PD-L1	Cancer
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .

HY-P1076

CALP2	Calmodulin	Inflammation/Immunology
CALP2 is a calmodulin (CaM) antagonist ( (K_d of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca ²⁺-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca ²⁺ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages .

HY-P1812A

AUNP-12 TFA NP-12 TFA	PD-1/PD-L1	Cancer
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .

HY-P1076A

CALP2 TFA	Calmodulin	Inflammation/Immunology
CALP2 TFA is a calmodulin (CaM) antagonist (K_d of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca ²⁺-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca ²⁺ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages .

HY-P5306

α-Conotoxin TxID	nAChR	Neurological Disease
α-Conotoxin TxID is a potent α3β4 nAChR antagonist with an IC₅₀ value of 12.5 nM. α-Conotoxin TxID has weak inhibition activity of closely related α6/α3β4 nAChR (IC₅₀= 94 nM). α-Conotoxin TxID has the potential for novel smoking cessation drug development .

HY-P5846

Muscarinic toxin 3 MT3	mAChR Adrenergic Receptor	Neurological Disease
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC₅₀s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M₁, M₄, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

HY-P1320

[Nphe1]Nociceptin(1-13)NH2	Opioid Receptor	Inflammation/Immunology
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pK_i=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA₂=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .

HY-P1320A

[Nphe1]Nociceptin(1-13)NH2 TFA	Opioid Receptor	Inflammation/Immunology
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pK_i=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA₂=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .

HY-P0299A

LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) Maximum Cited Publications 10 Publications Verification	TGF-β Receptor	Cancer
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .

HY-P1110

AF12198 1 Publications Verification	Interleukin Related	Inflammation/Immunology
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC₅₀=8 nM) but not the human type II receptor (IC₅₀=6.7 µM) or the murine type I receptor (IC₅₀>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC₅₀=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC₅₀=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .

HY-P0299

LSKL, Inhibitor of Thrombospondin (TSP-1) Maximum Cited Publications 10 Publications Verification	TGF-β Receptor	Cancer
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .

HY-103544

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P	JNK Interleukin Related Bombesin Receptor	Inflammation/Immunology Cancer
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca ²⁺ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer

Cat. No.	Product Name	Target	Research Area

HY-P99420

Acazicolcept ALPN-101	CD28	Inflammation/Immunology
Acazicolcept (ALPN-101), an Fc fusion protein, is a dual inducible T cell costimulator (ICOS)/CD28 antagonist. Acazicolcept has anti-inflammatory activities .

HY-P99168

Anifrolumab	Inhibitory Antibodies	Inflammation/Immunology
Anifrolumab is a type I interferon (IFN) receptor antagonist, a human monoclonal antibody. Anifrolumab blocks the activity of type I interferon. Anifrolumab can be used in systemic lupus erythematosus (SLE) research .

HY-P99111

Golimumab CNTO-148	TNF Receptor Apoptosis Interleukin Related Caspase	Inflammation/Immunology Cancer
Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research .

HY-P990032

Belrestotug EOS-448; EOS884448; GSK4428859A	Inhibitory Antibodies	Cancer
Belrestotug (EOS-448) is an antagonistic anti-TIGIT (VSIG9, VSTM3) human immunoglobulin G1 kappa (hIgG1 kappa) antibody. Belrestotug shows antineoplastic activity .

Cat. No.	Product Name	Chemical Structure

HY-14542S

Ziprasidone-d8
Ziprasidone-d₈8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.

HY-B1448AS

(Rac)-Benidipine-d7
(Rac)-Benidipine-d₇ is the deuterium labeled Benidipine[1]. Benidipine is a potent and orally active calcium channel antagonist[2]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[3]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[4].

HY-B0431AS

Phenoxybenzamine-d5 hydrochloride
Phenoxybenzamine-d₅ (hydrochloride) is the deuterium labeled Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity[1][2][3].

HY-B0431S

Phenoxybenzamine-d5
Phenoxybenzamine-d₅ is the deuterium labeled Phenoxybenzamine[1]. Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[2][3].

HY-100760S

Toxoflavin-13C4
Toxoflavin- ¹³C₄ is the ¹³C-labeled Toxoflavin. Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity[1][2]. Antibiotic properties.

HY-N0382S

Galangin-13C3
Galangin- ¹³C₃ is the ¹³C-labeled Galangin. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.

HY-14289S

Cimetidine-d3
Cimetidine-d₃ is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity[1][2][5].

HY-B0274AS

Chlorprothixene-d6 hydrochloride
Chlorprothixene-d₆ (hydrochloride) is the deuterium labeled Chlorprothixene hydrochloride. Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].

HY-B0539S

Desloratadine-d4
Desloratadine-d₄ is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].

HY-B0539S1

Desloratadine-d9
Desloratadine-d₉ is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].

HY-B0539S3

Desloratadine-d5
Desloratadine-d₅ is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].

HY-13004S

Maraviroc-d6

Maraviroc-d₆ (UK-427857-d6) is the deuterium labeled Maraviroc. Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV[1][2].

HY-B0431AS1

Phenoxybenzamine (benzyl-2,3,4,5,6-d5) (hydrochloride)
Phenoxybenzamine (benzyl-2,3,4,5,6-d₅) (hydrochloride) is the deuterium labeled Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity[1][2][3].

HY-139145S

Etbicyphat-13C3
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].

HY-B0539S2

Desloratadine-3,3,5,5-d4
Desloratadine-3,3,5,5-d₄ is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].

HY-B1396S

Nefazodone-d6 hydrochloride
Nefazodone-d₆ (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-B1396S1

Nefazodone-d6 dihydrochloride
Nefazodone-d₆ (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-N0368S

Linalool-d3
Linalool-d₃ is the deuterium labeled Linalool[1]. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity[2].Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome[3].

HY-14264S

Cyamemazine-d6
Cyamemazine-d₆ is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].

HY-16474S

Relugolix-d6

Relugolix-d₆ is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].

HY-B0461S

Trospium-d8 chloride
Trospium-d₈ (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].

HY-B0358AS

Flunarizine-d8 dihydrochloride
Flunarizine-d₈ dihydrochloride is deuterated labeled Flunarizine dihydrochloride (HY-B0358A). Flunarizine dihydrochloride is a potent dual Na ⁺/Ca ²⁺ channel (T-type) blocker. Flunarizine dihydrochloride is a D₂ dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .

HY-14940S

Volinanserin-d4 hydrochloride
Volinanserin-d₄ (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].

HY-15780S1

Brexpiprazole-d8-1

Brexpiprazole-d₈-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].

HY-B0539S4

Desloratadine-d4 hydrobromide
Desloratadine-d₄ hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .

HY-B0982S

Pindolol-d7
Pindolol-d₇ (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33 nM)[1][2].

HY-14914S1

Azilsartan-d4
Azilsartan-d₄ is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].

HY-W010201S

Citronellol-d6

Citronellol-d₆ is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities .

HY-17037S1

Pirenzepine-d8 dihydrochloride

Pirenzepine-d₈ (LS 519-d₈; Pirenzepin-d₈) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .

HY-A0027AS

Fenspiride-d5

Fenspiride-d₅ is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].

HY-W010410S

Oct-1-en-3-ol-d3

Oct-1-en-3-ol-d₃ is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities .

HY-B0965AS

Thioridazine-d3 hydrochloride

Thioridazine-d₃ (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].

HY-17387S1

(-)-Huperzine A-d4 hydrochloride

(-)-Huperzine A-d₄ hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC₅₀ of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .

HY-B0809S1

Theophylline-d3

Theophylline-d₃ is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research .

HY-B0203BS2

(Rac)-Nebivolol-d2,15N

(Rac)-Nebivolol-d₂, ¹⁵N is ¹⁵N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC₅₀ value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .

HY-W754151

N-Desmethyl apalutamide-d4

N-Desmethyl apalutamide-d₄ is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

HY-B0267BS

Oxybutynin-d5 hydrochloride

Oxybutynin-d₅ hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-12765S1

Losartan carboxylic acid-d4 hydrochloride

Losartan carboxylic acid-d₄ (hydrochloride) is deuterium labeled Losartan Carboxylic Acid. Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].

HY-B0822S1

Fipronil-13C6

Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

HY-14153S

Tegaserod-d11

Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

Cat. No.	Product Name		Classification

HY-151391

LPA5 antagonist 1		Alkynes
LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC₅₀=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research . LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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