Search Result
Results for "
convertases
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P2237
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-
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- HY-P5272
-
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Bacterial
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Inflammation/Immunology
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Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
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- HY-12402
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PCSK9
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Cardiovascular Disease
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SBC-115076 is a potent proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PCSK9 is a proprotein convertase, which plays a crucial role in LDL receptor metabolism .
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- HY-P1028
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Furin Inhibitor II
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Bacterial
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Infection
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Hexa-D-arginine (Furin Inhibitor II) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo .
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- HY-101832
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- HY-P2276A
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- HY-118120
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2-Guanidinoethylmercaptosuccinic acid
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Others
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Neurological Disease
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GEMSA is a potent inhibitor of enkephalin convertase (Ki=8.8 nM). GEMSA elicites analgesia .
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- HY-153451
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PCSK9
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Metabolic Disease
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PCSK9-IN-15 (compound 5) is a potent inhibitor of proprotein convertase subtilisin/kexin 9 (PCSK9, KD <200 nM). PCSK9 is involved in cholesterol metabolism and regulates levels of low-density lipoprotein cholesterol (LDL-C) in the blood. PCSK9- in -15 can be used to study cholesterol-lowering and dyslipidemia .
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- HY-P1028A
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Furin Inhibitor II TFA
|
Bacterial
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Infection
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Hexa-D-arginine TFA (Furin Inhibitor II TFA) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine TFA blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo .
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- HY-141724
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PCSK9
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Cancer
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PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. PCSK9 ligand 1 does not affect PCSK9 function .
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- HY-158825
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CIVI007 sodium
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PCSK9
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Metabolic Disease
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Cepadacursen sodium is a liver-targeting antisense oligonucleotide (ASO), inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) protein synthesis. Cepadacursen sodium can be used for hypercholesterolemia treatment and the prevention of atherosclerotic cardiovascular disease (ASCVD).
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- HY-153098
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-
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- HY-153098A
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Complement System
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Inflammation/Immunology
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ARC186 (sodium) is an unconjugated 40KDa PEG aptamer with a sequence identical to HY-147080 Avacincaptad pegol (ARC1905) sodium. ARC1905 is highly potent complement inhibitors that function by blocking the convertase-catalyzed activation of C5.
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- HY-120088A
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PCSK9
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Cardiovascular Disease
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PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34 .
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- HY-120088
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PCSK9
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Cardiovascular Disease
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PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region .
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- HY-112598
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PCSK9
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Metabolic Disease
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PF-06815345 is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 significantly decreases the PCSK9 level in vivo in mouse .
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- HY-112598A
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PCSK9
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Cardiovascular Disease
Metabolic Disease
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PF-06815345 hydrochloride is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 hydrochloride significantly decreases the PCSK9 level in vivo in mouse .
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- HY-P99050
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-
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- HY-148687
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PCSK9
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Cardiovascular Disease
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SPC5001 is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′ .
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- HY-148687A
-
|
PCSK9
|
Cardiovascular Disease
|
SPC5001 sodium is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 sodium can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′ .
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- HY-158827
-
|
PCSK9
|
Metabolic Disease
|
AZD8233, a liver-targeting antisense oligonucleotide (ASO), inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) protein synthesis. AZD8233 increases the available LDL receptors by reducing PCSK9 levels, thereby clearing LDL from the blood and decreasing LDL-C levels.
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-
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- HY-130245
-
|
PCSK9
|
Metabolic Disease
|
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
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-
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- HY-N10702
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PCSK9
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Cardiovascular Disease
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PCSK9-IN-9 is an isocoumarins of natural origin. PCSK9-IN-9 can inhibit proprotein convertase subtilisin-kexin type 9 (PCSK9), IDOL, and SREBP2 mRNA expression. PCSK9-IN-9 inhibits PCSK9 with an IC50 value of 11.9 μM .
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- HY-153785
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Complement System
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Inflammation/Immunology
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NH2-C6-ARC186 sodium is a modified ARC186 (HY-153098) with NH2-C6 that can be coupled to other peptides or molecules. ARC186 is a aptamer and a highly potent complement inhibitor that function by blocking the convertase-catalyzed activation of C5 .
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- HY-128342
-
|
Complement System
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Inflammation/Immunology
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Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM .
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-
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- HY-P9928A
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REGN 727(anti-PCSK9); SAR 236553(anti-PCSK9)
|
PCSK9
|
Cardiovascular Disease
Cancer
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Alirocumab (anti-PCSK9) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia .
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- HY-P990091
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SAR 445088
|
Complement System
|
Inflammation/Immunology
|
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .
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- HY-130245A
-
|
PCSK9
|
Metabolic Disease
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(R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
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- HY-P990025
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ARGX-117
|
Complement System
|
Inflammation/Immunology
|
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .
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-
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- HY-130666
-
|
Endogenous Metabolite
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Cardiovascular Disease
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Chlorambucyl-proline is a chloroplatinyl amino acid derivative with inhibitory activity against bovine pulmonary vasoconstrictor enzyme. Chlorambucyl-proline reacts with the convertase in a 1:1 ratio, and the removal of its radiolabel indicates that the compound has an irreversible inhibitory effect on the enzyme activity. Chlorambucyl-proline binds to the aspartic acid or glutamic acid side chain of the enzyme by forming an ester bond, resulting in irreversible inactivation of the enzyme. The inactivation rate constant of chlororambucyl-proline increases in the pH range of 5-8, indicating that its effect on the enzyme activity is affected by the pH environment .
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- HY-P99965
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SKY59; RO7112689
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Complement System
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Cardiovascular Disease
Metabolic Disease
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Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2237
-
-
- HY-P5272
-
|
Bacterial
|
Inflammation/Immunology
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
-
- HY-P1028
-
Furin Inhibitor II
|
Bacterial
|
Infection
|
Hexa-D-arginine (Furin Inhibitor II) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo .
|
-
- HY-P2276A
-
-
- HY-P1028A
-
Furin Inhibitor II TFA
|
Bacterial
|
Infection
|
Hexa-D-arginine TFA (Furin Inhibitor II TFA) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine TFA blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo .
|
-
- HY-P5970
-
TACE Substrate
|
Peptides
|
Cancer
|
DABCYL-TNF-α-EDANS (-4 to +6) (human) is a FRET peptide substrate of tumor necrosis factor convertase (TACE) .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99050
-
-
- HY-P9928A
-
REGN 727(anti-PCSK9); SAR 236553(anti-PCSK9)
|
PCSK9
|
Cardiovascular Disease
Cancer
|
Alirocumab (anti-PCSK9) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia .
|
-
- HY-P990091
-
SAR 445088
|
Complement System
|
Inflammation/Immunology
|
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .
|
-
- HY-P990025
-
ARGX-117
|
Complement System
|
Inflammation/Immunology
|
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .
|
-
- HY-P99965
-
SKY59; RO7112689
|
Complement System
|
Cardiovascular Disease
Metabolic Disease
|
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
|
Classification |
-
- HY-148687A
-
|
|
Antisense Oligonucleotides
|
SPC5001 sodium is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 sodium can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′ .
|
-
- HY-153785
-
|
|
Aptamers
|
NH2-C6-ARC186 sodium is a modified ARC186 (HY-153098) with NH2-C6 that can be coupled to other peptides or molecules. ARC186 is a aptamer and a highly potent complement inhibitor that function by blocking the convertase-catalyzed activation of C5 .
|
-
- HY-158825
-
CIVI007 sodium
|
|
Antisense Oligonucleotides
|
Cepadacursen sodium is a liver-targeting antisense oligonucleotide (ASO), inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) protein synthesis. Cepadacursen sodium can be used for hypercholesterolemia treatment and the prevention of atherosclerotic cardiovascular disease (ASCVD).
|
-
- HY-153098
-
|
|
Aptamers
|
ARC186 (sodium) is an unconjugated 40KDa PEG aptamer with a sequence identical to HY-147080 Avacincaptad pegol (ARC1905) sodium. ARC1905 is highly potent complement inhibitors that function by blocking the convertase-catalyzed activation of C5.
|
-
- HY-148687
-
|
|
Antisense Oligonucleotides
|
SPC5001 is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′ .
|
-
- HY-158827
-
|
|
Antisense Oligonucleotides
|
AZD8233, a liver-targeting antisense oligonucleotide (ASO), inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) protein synthesis. AZD8233 increases the available LDL receptors by reducing PCSK9 levels, thereby clearing LDL from the blood and decreasing LDL-C levels.
|
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