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dissociation rates

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By Targets:	Adenosine Receptor (1) Adenylate Cyclase (1) Endogenous Metabolite (1) HDAC (1) Na+/K+ ATPase (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Metabolic Disease (1)

5

Inhibitors & Agonists

2

Peptides

2

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

TDI-11861	Adenylate Cyclase	Others
TDI-11861 is second-generation soluble Adenylyl Cyclase (sAC, ADCY10) inhibitor with slow dissociation rates. TDI-11861 inhibits sAC cellular with an IC₅₀ value of 5.5 nM .

Coumarin-SAHA	HDAC	Cancer
Coumarin-SAHA is a fluorescent probe for determining the binding affinities (k_d) and the dissociation off-rates (k_off) of the HDAC8-inhibitor complexes .

MRS8247	Adenosine Receptor	Others
MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) that can also slow the dissociation rate of agonists .

(6S)-Tetrahydrofolic acid (6S)-5,6,7,8-Tetrahydrofolic acid	Endogenous Metabolite	Metabolic Disease
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .

SC4453	Na+/K+ ATPase	Cardiovascular Disease
SC4453 is a digoxin analogue in which the lactone ring at C17β is replaced by a pyrazine ring. SC4453 is slightly inferior to digoxin in inhibiting (Na+ + K+)-ATPase, but shows similar sensitivity to potassium ions. The differences in the sensitivity of SC4453 to heart and brain tissue from different species are mainly due to differences in its dissociation rate from the receptor. These observations confirm the high sensitivity of the human heart to cardiac glycosides.

Cat. No.	Product Name	Target	Research Area

GPR110 peptide agonist P12 acetate	Peptides	Cancer
GPR110 peptide agonist P12 acetate is the acetate salt form of GPR110 peptide agonist P12 (HY-P10495). GPR110 peptide agonist P12 acetateis a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 acetate can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 acetate mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 acetate can be used in the study of developmental disorders and cancers related to GPR110 .

GPR110 peptide agonist P12	Peptides	Others Cancer
GPR110 peptide agonist P12 is a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 can be used in the study of developmental disorders and cancers related to GPR110 .

Cat. No.	Product Name	Category	Target	Chemical Structure

(6S)-Tetrahydrofolic acid (6S)-5,6,7,8-Tetrahydrofolic acid	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	Endogenous Metabolite
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .

SC4453	Triterpenes Structural Classification Animals Terpenoids Source classification	Na+/K+ ATPase
SC4453 is a digoxin analogue in which the lactone ring at C17β is replaced by a pyrazine ring. SC4453 is slightly inferior to digoxin in inhibiting (Na+ + K+)-ATPase, but shows similar sensitivity to potassium ions. The differences in the sensitivity of SC4453 to heart and brain tissue from different species are mainly due to differences in its dissociation rate from the receptor. These observations confirm the high sensitivity of the human heart to cardiac glycosides.

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