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less-active

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By Targets:	5-HT Receptor (2) Acetyl-CoA Carboxylase (1) Adrenergic Receptor (3) Amyloid-β (1) Androgen Receptor (1) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (1) Apoptosis (3) Autophagy (2) Bacterial (3) Bcl-2 Family (2) Beta-secretase (1) Biochemical Assay Reagents (2) Btk (2) Calcium Channel (5) Carbonic Anhydrase (1) CDK (1) ClpP (1) COX (1) CRM1 (1) Dipeptidyl Peptidase (2) Dopamine Receptor (1) Drug Isomer (2) Drug Metabolite (1) EGFR (2) Elastase (2) Epigenetic Reader Domain (4) Estrogen Receptor/ERR (2) Eukaryotic Initiation Factor (eIF) (1) Farnesyl Transferase (1) FLT3 (1) Fungal (2) GABA Receptor (1) Glucocorticoid Receptor (1) GSK-3 (1) HBV (3) HDAC (1) Histamine Receptor (1) Histone Demethylase (1) Histone Methyltransferase (2) HIV (2) IFNAR (2) iGluR (2) IKK (1) Insecticide (1) Isocitrate Dehydrogenase (IDH) (3) Isotope-Labeled Compounds (2) JAK (5) JNK (1) Keap1-Nrf2 (1) Lactate Dehydrogenase (1) MEK (1) MetAP (1) mGluR (3) Monoamine Oxidase (2) nAChR (1) Neurokinin Receptor (1) NF-κB (2) Opioid Receptor (2) P2X Receptor (1) Parasite (1) PD-1/PD-L1 (1) Phosphodiesterase (PDE) (1) PI3K (2) Polo-like Kinase (PLK) (1) Prostaglandin Receptor (2) Ras (1) Reactive Oxygen Species (1) RSV (1) Sodium Channel (2) STING (1) Tie (1) Toll-like Receptor (TLR) (2) Tyrosinase (1) Virus Protease (1) Wee1 (1)
By Research Areas:	Cancer (39) Cardiovascular Disease (7) Endocrinology (4) Infection (13) Inflammation/Immunology (22) Metabolic Disease (8) Neurological Disease (24)
Click Chemistry:	Alkynes (1)

118

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15084A

(-)-Dizocilpine maleate (-)-MK-801 maleate	iGluR	Neurological Disease
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a K_i of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .

HY-15652

Freselestat ONO-6818; ONO-PO-736	Elastase	Inflammation/Immunology
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a K_i of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .

HY-14864A

(S)-Mapracorat (S)-ZK-245186; (S)-BOL-303242X	Glucocorticoid Receptor	Endocrinology
(S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.

HY-13735C

l-Atabrine dihydrochloride	Bacterial	Infection
l-Atabrine dihydrochloride is a less active enantiomer of quinacrine which displays antiprion activity.

HY-17044A

Duvelisib (R enantiomer) IPI-145 R enantiomer; INK1197 R enantiomer	PI3K	Cancer
Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.

HY-13079

Cobimetinib (R-enantiomer) GDC-0973 (R-enantiomer); XL-518 (R-enantiomer)	MEK	Cancer
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

HY-100029B

*Bay 41-4109 (less active* enantiomer)**	HBV	Infection
Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC₅₀ of 53 nM.

HY-126047B

(R)-(+)-Anatabine	NF-κB Amyloid-β nAChR	Neurological Disease Inflammation/Immunology
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .

HY-15652A

Freselestat quarterhydrate ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate	Elastase	Inflammation/Immunology
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a K_i of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .

HY-14645B

DHMEQ racemate rel-DHMEQ	NF-κB	Cancer
DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ.

HY-124909

(6R)-FR054	Apoptosis	Cancer
(6R)-FR054 is a less active isomer of FR054.

HY-125784A

(R)-Viloxazine hydrochloride	5-HT Receptor	Neurological Disease
(R)-Viloxazine hydrochloride is a less active R-isomer of Viloxazine hydrochloride. Viloxazine hydrochloride is an effective antidepressant agent .

HY-U00008

CP-28888 CP 28888-27	IFNAR	Infection
CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.

HY-100423A

Eltanexor Z-isomer 1 Publications Verification KPT-8602 (Z-isomer)	CRM1	Cancer
Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.

HY-12872B

Nazartinib S-enantiomer EGF816 (S-enantiomer)	EGFR	Others
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.

HY-120813A

ARN 077 (enantiomer) URB913 (enantiomer)	Drug Isomer	Inflammation/Immunology
ARN 077 enantiomer (19) is the less active enantiomer of ARN 077, with an IC₅₀ of 3.53 μM for rat NAAA .

HY-145009

SN-008	STING	Others
SN-008, a less active SN-011 analog, can be used as a negative control .

HY-114673

Benzomalvin B	Neurokinin Receptor	Others
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P .

HY-18767A

(R,S)-Ivosidenib 1 Publications Verification (R,S)-AG-120	Isocitrate Dehydrogenase (IDH)	Cancer
(R,S)-Ivosidenib ((R,S)-AG-120) is the less active enantiomer of Ivosidenib (AG-120) .

HY-100742B

(S)-GNE-140	Lactate Dehydrogenase	Cancer
(S)-GNE-140 is the less active enantiomer of GNE-140 which can inhibit Lactate dehydrogenase A (LDHA).

HY-N0756A

(-)-Bornyl acetate L-(-)-Bornyl acetate	Fungal	Infection
(-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .

HY-16901A

Firsocostat (S enantiomer) ND-630 (S enantiomer); GS-0976 (S enantiomer); NDI-010976 (S enantiomer)	Acetyl-CoA Carboxylase	Others
Firsocostat S enantiomer (ND-630 S enantiomer) is the less active S enantiomer of Firsocostat. Firsocostat is an acetyl-CoA carboxylase (ACC) inhibitor.

HY-14855A

(S)-Tedizolid 2 Publications Verification (S)-TR 700; (S)-DA 7157	Bacterial Antibiotic	Infection
(S)-Tedizolid is the S-enantiomer of Tedizolid. Tedizolid is a novel oxazolidinone with activity against Gram-positive pathogens. (S)-Tedizolid is the less active isomer.

HY-B2111

(R)-(+)-Atenolol	Adrenergic Receptor	Cardiovascular Disease Others
(R)-(+)-Atenolol is the less active enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a β-adrenergic receptor antagonist .

HY-15853A

MK-7246 S enantiomer	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
MK-7246 S enantiomer is the less active enantiomer of MK-7246. MK-7246 is a potent and selective CRTH2 antagonist.

HY-40354B

(3S,4R)-Tofacitinib	JAK	Inflammation/Immunology
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

HY-40354D

(3R,4S)-Tofacitinib	JAK	Inflammation/Immunology
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

HY-10502A

Tipifarnib (S enantiomer) IND-58359 S enantiomer; (S)-(-)-R-115777	Farnesyl Transferase	Cancer
Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC₅₀ of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.

HY-16950B

(E)-4-Hydroxytamoxifen (E)-Afimoxifene	Estrogen Receptor/ERR	Cancer
(E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.

HY-112218A

(R)-MIK665	Bcl-2 Family	Cancer
(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC₅₀ of 1.81 nM.

HY-12279F

Umbralisib R-enantiomer TGR-1202 R-enantiomer; RP5264 R-enantiomer	PI3K	Cancer
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.

HY-40354C

(3S,4S)-Tofacitinib	JAK	Inflammation/Immunology
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

HY-12993B

RSV604 (R enantiomer) A-60444 (R enantiomer)	RSV	Infection
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.

HY-101281B

(R)-VU 6008667	Others	Neurological Disease
(R)-VU 6008667, the less active (R)-enantiomer to VU 6008667, is devoid of M5 NAM activity (IC₅₀>10 μM) .

HY-112895A

(R)-UT-155	Androgen Receptor	Cancer
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer .

HY-B0106A

Etiracetam UCB 6474	Calcium Channel	Neurological Disease
Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .

HY-100664

Zopiclone N-oxide RP 29753	Drug Metabolite GABA Receptor	Neurological Disease
Zopiclone N-oxide (RP 29753) is a less active metabolite of Zopiclone. Zopiclone N-oxide is also an impurity of Eszopiclone and is formed by the oxidation of Eszopiclone .

HY-18715

Ornidazole (Levo-) (S)-Ornidazole; Levornidazole	Bacterial Parasite	Infection
Ornidazole Levo- is the levo-isomer of Ornidazole. Ornidazole is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Ornidazole Levo- is the less active isomer.

HY-12481A

SAR405 R enantiomer	Others	Cancer
SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.

HY-W074930

(S)-Tenofovir (S)-GS 1278; (S)-PMPA; (S)-TDF	HIV HBV	Infection
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV) .

HY-50949A

Bay 65-1942 (R form)	IKK	Inflammation/Immunology
Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.

HY-12305A

(R)-Q-VD-OPh (R)-QVD-OPH; (R)-Quinoline-Val-Asp-Difluorophenoxymethylketone	Apoptosis	Cancer
(R)-Q-VD-OPh ((R)-QVD-OPH) is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible pan-caspase inhibitor with potent antiapoptotic properties.

HY-13749C

(S)-Sitagliptin phosphate (S)-MK-0431 phosphate	Dipeptidyl Peptidase Autophagy	Metabolic Disease
(S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC₅₀ of 19 nM in Caco-2 cell extracts .

HY-100540C

Golgicide A-1 GCA-1	Drug Isomer	Infection
Golgicide A-1 (GCA-1) is a less active cis-diastereomer of Golgicide A (GCA). Golgicide A-1 weakly inhibits mosquito reproduction .

HY-114277B

Sotorasib isomer AMG-510 isomer	Others	Others
Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.

HY-U00417

ARS-1630	Ras	Cancer
ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.

HY-122808

(-)-Camphoric acid	mGluR	Metabolic Disease
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1 .

HY-19414A

(R)-MLN-4760	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
(R)-MLN-4760, the R-enantiomer of MLN-4760, is an ACE2 inhibitor, with an IC₅₀ of 8.4 μM. (R)-MLN-4760 is the less active isomer .

HY-122167

L-869298	Phosphodiesterase (PDE)	Inflammation/Immunology
L-869298 is a potent and selective PDE4 inhibitor with an IC₅₀ of 0.5 nM for PDE4A. L-869298 shows less active against hERG potassium channel .

HY-W067479

(E)-Cinnamamide	Insecticide	Others
(E)-Cinnamamide, the less active isomer of Cinnamamide. Cinnamamide, a derivative of the plant secondary compound Cinnamic acid. Cinnamamide is effective as a non-lethal chemical repellent suitable for reducing avian pest damage .

Cat. No.	Product Name	Type

HY-120973

Butaprost free acid

Biochemical Assay Reagents

(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)

Cat. No.	Product Name	Target	Research Area

HY-P2678

CCK (26-31) (non-sulfated)	Peptides	Metabolic Disease
CCK (26-31) (non-sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety. CCK (26-31) is also less active in non-sulfated than in sulfated form .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0756A

(-)-Bornyl acetate L-(-)-Bornyl acetate	Infection Structural Classification Natural Products other families Classification of Application Fields Source classification Plants Disease Research Fields	Fungal
(-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .

HY-122808

(-)-Camphoric acid	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Cinnamomum glanduliferum (Wall.) Nees Metabolic Disease Plants Lauraceae Disease Research Fields	mGluR
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1 .

HY-W067479

(E)-Cinnamamide	Structural Classification Simaroubaceae Classification of Application Fields Simple Phenylpropanols Source classification Other Diseases Phenylpropanoids Plants Disease Research Fields Picrasma quassioides(D．Don)Benn．	Insecticide
(E)-Cinnamamide, the less active isomer of Cinnamamide. Cinnamamide, a derivative of the plant secondary compound Cinnamic acid. Cinnamamide is effective as a non-lethal chemical repellent suitable for reducing avian pest damage .

HY-N1778A

(E)-3,4-Dimethoxycinnamic acid (E)-O-Methylferulic acid	Infection Structural Classification other families Classification of Application Fields Ketones, Aldehydes, Acids Source classification Plants Disease Research Fields	Reactive Oxygen Species Virus Protease
(E)-3,4-Dimethoxycinnamic acid is the less active isomer of 3,4-Dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway . Anti-apoptotic effects .

HY-N0136B

(-)-Taxifolin (-)-Dihydroquercetin	Flavanonols Flavonoids other families Classification of Application Fields Source classification Phenols Polyphenols Plants Disease Research Fields Inflammation/Immunology	Tyrosinase
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC₅₀ value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .

HY-114673

Benzomalvin B	Alkaloids Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Source classification Other Diseases Quinoline Alkaloids Endogenous metabolite Disease Research Fields	Neurokinin Receptor
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P .

HY-N0756AR

(-)-Bornyl acetate (Standard)	Structural Classification Natural Products other families Source classification Plants	Fungal
(-)-Bornyl acetate (Standard) is the analytical standard of (-)-Bornyl acetate. This product is intended for research and analytical applications. (-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .

Cat. No.	Product Name	Chemical Structure

HY-16950BS

(E)-4-Hydroxytamoxifen-d5
(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.

HY-B0106AS

Etiracetam-d3
Etiracetam-d₃ is the deuterium labeled Etiracetam. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059)[1].

Cat. No.	Product Name		Classification

HY-13728A

(R)-Plevitrexed (R)-ZD 9331; (R)-BGC9331		Alkynes
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed 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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less-active

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

Natural
Products