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AB141167

Gabexate mesylate, General serine protease inhibitor

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MW 417.5 Da, Purity >99%. General serine protease inhibitor (Ki values are 3.4 nM, 5, 1.8 μM and 2.6 mM at tryptase, thrombin, tyrpsin and kallikrein serine proteases respectively). Additionally inhibits nitric oxide synthase. Displays antithrombotic activity and antitumor effect. Active in vivo.

View Alternative Names

Atherosclerosis, susceptibility to, included, CP2D6_HUMAN, CPD6, CYP2D, CYP2D7AP, CYP2D7BP, CYP2D7P2, CYP2D8P2, CYP2DL1, CYPIID6, Cholesterol 25-hydroxylase, Chymotryptic stratum corneum, Cytochrome P450 2D6, Cytochrome P450 family 2 subfamily D member 6, Cytochrome P450 family 2 subfamily D polypeptide 6, Cytochrome P450-DB1, DKFZp686N23123, Debrisoquine 4-hydroxylase, ER, ER-alpha, ER-beta, ER[a], ER[b], ESR, ESR B, ESR BETA, ESR1_HUMAN, ESRA, ESTR B, Era, Erb, Erb2, Estr, Estra, Estradiol Receptor alpha, Estradiol Receptor beta, Estradiol receptor, Estrogen Receptor 1, Estrogen Receptor 2, Estrogen receptor, Estrogen receptor 1 (alpha), Estrogen receptor 2 (ER beta), Estrogen receptor 2 ER beta, Estrogen receptor alpha, Estrogen receptor beta 4, Estrogen resistance, included, HDL cholesterol, augmented response of, to hormone replacement, included, KLK7_HUMAN, Kallikrein 7 (chymotryptic stratum corneum), Kallikrein related peptidase 7, Kallikrein-7, Microsomal monooxygenase, Myocardial infarction, susceptibility to, included, NR3A1, NR3A2, Nuclear receptor subfamily 3 group A member 1, Nuclear receptor subfamily 3 group A member 2, OTTHUMP00000017718, OTTHUMP00000017719, P450 DB1, P450C2D, PRSS 6, Protease serine 6, RNESTROR, SCCE, Serine protease 6, Signal protein, Stratum corneum chymotryptic enzyme, Xenobiotic monooxygenase, flavoprotein-linked monooxygenase, hK 7, hSCCE

1 Images
Chemical Structure - Gabexate mesylate, General serine protease inhibitor (AB141167)
  • Chemical Structure

Lab

Chemical Structure - Gabexate mesylate, General serine protease inhibitor (AB141167)

2D chemical structure image of ab141167, Gabexate mesylate, General serine protease inhibitor

Key facts

CAS number

56974-61-9

Purity

>99%

Form

Solid

form

Molecular weight

417.5 Da

Molecular formula

C<sub>1</sub><sub>7</sub>H<sub>2</sub><sub>7</sub>N<sub>3</sub>O<sub>7</sub>S

PubChem

6604561

Nature

Synthetic

Solubility

Soluble in water to 100 mM

Biochemical name

Gabexate mesylate

Biological description

General serine protease inhibitor (Ki values are 3.4 nM, 5, 1.8 μM and 2.6 mM at tryptase, thrombin, tyrpsin and kallikrein serine proteases respectively). Additionally inhibits nitric oxide synthase. Displays antithrombotic activity and antitumor effect. Active in vivo.

Canonical smiles

CCOC(=O)C1=CC=C(C=C1)OC(=O)CCCCCN=C(N)N.CS(=O)(=O)O

InChi

InChI=1S/C16H23N3O4.CH4O3S/c1-2-22-15(21)12-7-9-13(10-8-12)23-14(20)6-4-3-5-11-19-16(17)18;1-5(2,3)4/h7-10H,2-6,11H2,1H3,(H4,17,18,19);1H3,(H,2,3,4)

InChiKey

DNTNDFLIKUKKOC-UHFFFAOYSA-N

IUPAC Name

ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate;methanesulfonic acid

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Estrogen receptor also known as ER functions as a ligand-activated transcription factor. This receptor binds estrogens such as estradiol and regulates gene expression by interacting with specific DNA sequences. It weighs approximately 66 kilodaltons and is mainly expressed in reproductive tissues like the ovaries and uterus as well as in breast tissue. CYP2D6 is a cytochrome P450 enzyme part of a superfamily involved in the metabolism of medications. Weighing around 55 kilodaltons CYP2D6 shows expression mostly in the liver and small intestine. Kallikrein 7 or KLK7 acts as a serine protease that plays a role in skin desquamation with a mass of about 29 kilodaltons and expression found in the skin and other epithelial tissues.
Biological function summary

The estrogen receptor influences the growth and function of reproductive tissues and also plays a role in bone density maintenance. It can form complexes with co-activators for transcriptional activity. CYP2D6 is responsible for metabolizing approximately 25% of clinical drugs including antidepressants and opioids. It requires electron transfer from NADPH-cytochrome P450 reductase for its catalytic cycle. KLK7 breaks down corneodesmosomal proteins in the outer skin layers making it important for normal skin shedding. This protease does not act alone but rather as part of the kallikrein-related peptidase family.

Pathways

We see the estrogen receptor participating in the estrogen signaling pathway which is critical for sexual development and reproductive function. It interacts with co-regulators like steroid receptor coactivator-1 (SRC-1). CYP2D6 integrates into the drug metabolism pathway involving others like cytochrome P450 oxidoreductase to transform drugs into their active forms or prepare them for elimination. KLK7 participates in skin barrier formation and regulation pathways often interacting with other kallikrein-related peptidases in maintaining skin homeostasis and regulating inflammation.

Estrogen receptor's malfunction or aberrant expression links to breast cancer with overexpression often noted in hormone-receptor-positive types influencing tumor growth alongside HER2. CYP2D6 genetic polymorphisms can lead to altered drug metabolism affecting conditions like depression due to differential drug responses. KLK7 relates to atopic dermatitis where its increased activity may contribute to the disease's skin barrier dysfunction often alongside other proteases like KLK5. These associations highlight the importance of these targets in maintaining health or contributing to disease states.
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Product protocols

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