Adenylate-Cyclase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html Adenylate HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html CyclaseAdenylyl cyclaseAdenylyl cyclases (ACs) are enzymes that catalyze the production of cyclic adenosin

2、e monophosphate (cAMP) from adenosinetriphosphate (ATP). Adenylyl cyclases integrate positive and negative signals that act through G protein-coupled cell-surfacereceptors with other extracellular stimuli to finely regulate levels of cAMP within the cell. Humans express nine isoforms ofmembranous AC

3、s and a soluble AC.Based on regulatory properties, transmembrane ACs are classified into four groups: Group I: Ca2+/calmodulin-stimulated AC1, AC3,AC8; Group II: G-stimulated and Ca2+-insensitive AC2, AC4, AC7; Group III: Gi/Ca2+/PKA-inhibited AC5, AC6; Group IV:forskolin/Ca2+/G-insensitive AC9. The

4、 soluble AC, unlike the transmembrane ACs, is insensitive to hormones, G proteins andforskolin, a diterpene extracted from the root of the plant Coleus forskohlii that directly activates all isoforms of transmembraneACs except AC9.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclas

5、e.html Adenylate HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html Cyclase HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html Inhibitors, HYPERLINK https:/ww

6、w.MedChemE/Targets/Adenylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html & HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html

7、HYPERLINK https:/www.MedChemE/Targets/Adenylate Cyclase.html Activators HYPERLINK https:/www.MedChemE/2-5-dideoxyadenosine.html 2,5-Dideoxyadenosine HYPERLINK https:/www.MedChemE/2-5-dideoxyadenosine.html HYPERLINK https:/www.MedChemE/ac1-in-1.html AC1-IN-1Cat. No.: HY-135878 Cat. No.: HY-1458302,5-

8、Dideoxyadenosine is a potent andnon-competitive adenylyl cyclase inhibitor viabinding the P-site with an IC of 3 M .502,5-Dideoxyadenosine is a nucleoside analog andexerts a potent antiadrenergic action in heart.AC1-IN-1 is a potent and selective Adenylyl cyclasetype 1 (AC1) inhibitor with an IC of

9、0.54 M.50AC1-IN-1 displays modest antiallodynic effects ina mouse model of inflammatory pain. AC1-IN-1 hasCNS activity.Purity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 250 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK h

10、ttps:/www.MedChemE/angiopeptin.html Angiopeptin HYPERLINK https:/www.MedChemE/angiopeptin.html HYPERLINK https:/www.MedChemE/angiopeptin-tfa.html Angiopeptin HYPERLINK https:/www.MedChemE/angiopeptin-tfa.html HYPERLINK https:/www.MedChemE/angiopeptin-tfa.html TFACat. No.: HY-P2090 Cat. No.: HY-P2090

11、AAngiopeptin, a cyclic octapeptide analogue ofsomatostatin, is a weak sst /sst receptor2 5partial agonist with IC values of 0.26nM and506.92nM, respectively.Angiopeptin TFA, a cyclic octapeptide analogue ofsomatostatin, is a weak sst /sst receptor2 5partial agonist with IC values of 0.26nM and506.92

12、nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.16%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/CB-7921220.html CB-7921220 HYPERLINK https:/www.MedChemE/CB-7921220.html HYPERLINK https:/www.MedChemE/Fipexide

13、.html FipexideCat. No.: HY-101862 Cat. No.: HY-B1124CB-7921220 is an adenylate cyclase inhibitor.Fipexide, a parachloro-phenossiacetic acidderivative, is a nootropic drug. Fipexide reducesstriatal adenylate cyclase activity. Fipexide haspositive effect on cognitive performance bydopaminergic neurotr

14、ansmission. Fipexide isused for senile dementia research.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.99%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/fipexide-hydrochloride.html Fipexide HYPERLINK http

15、s:/www.MedChemE/fipexide-hydrochloride.html HYPERLINK https:/www.MedChemE/fipexide-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/fipexide-hydrochloride.html HYPERLINK https:/www.MedChemE/Forskolin.html ForskolinCat. No.: HY-B1124A(Coleonol; Colforsin) Cat. No.: HY-15371Fipexide hydr

16、ochloride, aparachloro-phenossiacetic acid derivative, is anootropic drug. Fipexide hydrochloride reducesstriatal adenylate cyclase activity.Forskolin (Coleonol) is a potent adenylate cyclaseactivator with an IC of 41 nM and an of50 EC500.5 M for type I adenylyl cyclase. Forskolin isalso an inducer

17、of intracellular cAMPformation.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/guanylyl-imidodiphosphate-lithium.html Guanylyl HYPERLINK https:/www.MedChemE/guanylyl-imi

18、dodiphosphate-lithium.html HYPERLINK https:/www.MedChemE/guanylyl-imidodiphosphate-lithium.html imidodiphosphate HYPERLINK https:/www.MedChemE/guanylyl-imidodiphosphate-lithium.html HYPERLINK https:/www.MedChemE/guanylyl-imidodiphosphate-lithium.html lithium HYPERLINK https:/www.MedChemE/guanylyl-im

19、idodiphosphate-lithium.html HYPERLINK https:/www.MedChemE/KH7.html KH7(Gpp(NH)p lithium) Cat. No.: HY-137167Cat. No.: HY-103194Guanylyl imidodiphosphate (Gpp(NH)p) lithium, anon-hydrolyzable GTP analogue, increases adenylatecyclase activity.KH7 is a soluble adenylyl cyclase (sAC)-specificinhibitor,

20、with IC s of 3-10 M toward both50recombinant purified human sAC protein andtheterologously expressed sACt in cellular assays.KH7 is also a cAMP inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.19%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg

21、, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/LRE1.html LRE1Cat. No.: HY-100524 HYPERLINK https:/www.MedChemE/Lysipressin.html Lysipressin(Lysine vasopressin; Lys8-Vasopressin) Cat. No.: HY-P0004LRE1 is a specific and allosteric inhibi

22、tor ofsoluble adenylyl cyclase.Lysipressin is Antidiuretic hormone that have beenfound in pigs and some marsupial families. Inducescontraction of the rabbit urinary bladder smoothmuscle, activate adenylate-cyclase.Purity: 99.59%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50

23、mg, 100 mgPurity: 99.76%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/mant-gtps.html Mant-GTPSCat. No.: HY-115748 HYPERLINK https:/www.MedChemE/nb001.html NB001(HTS 09836) Cat. No.: HY-14425Mant-GTPS, a GTP mimetic, is a potent competitiveadenylyl cy

24、clase (AC) inhibitor. Mant-GTPS is apotent YdeH inhibitor.NB001 (HTS 09836) is an adenylcyclase 1 (AC1)inhibitor which has effect on neural andnon-neural pain by modulating AC1 activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.21%Clinical Data: No Development Repor

25、tedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nkh477.html NKH477(Colforsin dapropate hydrochloride) Cat. No.: HY-103193 HYPERLINK https:/www.MedChemE/nky80.html NKY80Cat. No.: HY-103195NKH477 (Colforsin dapropate hydrochloride)directly activates the catalytic unit of adenylatecyclase and increas

26、es intracellular cAMP. NKH477 isa forskolin derivative that improves cardiacfailure mainly through its beneficial effects ondiastolic cardiac function.NKY80 is a potent, selective and non-competitiveadenylyl cyclase (AC) type V isoform inhibitorwith IC s of 8.3 M, 132 M and 1.7 mM for type50V, III a

27、nd II, respectively. NKY80 is anon-nucleoside quinazolinone and regulates the ACcatalytic activity in heart and lung tissues.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 10

28、0 mg HYPERLINK https:/www.MedChemE/skf-83566.html SKF-83566 HYPERLINK https:/www.MedChemE/skf-83566.html HYPERLINK https:/www.MedChemE/skf-83566-hydrobromide.html SKF-83566 HYPERLINK https:/www.MedChemE/skf-83566-hydrobromide.html HYPERLINK https:/www.MedChemE/skf-83566-hydrobromide.html hydrobromid

29、eCat. No.: HY-103430A Cat. No.: HY-103430SKF-83566 is a potent, blood-brain permeableand orally active D1-like dopamine receptor(D1DR) antagonist and a weaker competitiveantagonist at the vascular 5-HT receptor2(K=11 nM).iPurity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

30、 mg, 25 mgSKF-83566 hydrobromide is apotent, blood-brain permeable and orallyactive D1-like dopamine receptor(D1DR) antagonist and a weaker competitiveantagonist at the vascular 5-HT receptor2(K=11 nM).iPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.Me

31、dChemE/Small_Cardioactive_Peptide_B_SCPB.html Small HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html Cardioactive HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html HYPERLINK https:/www.MedChem

32、E/Small_Cardioactive_Peptide_B_SCPB.html Peptide HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html B HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html HYPERLINK https:/www.MedChemE/Small_Cardio

33、active_Peptide_B_SCPB.html (SCPB) HYPERLINK https:/www.MedChemE/Small_Cardioactive_Peptide_B_SCPB.html HYPERLINK https:/www.MedChemE/SQ22536.html SQ22536Cat. No.: HY-P1495 Cat. No.: HY-100396Small Cardioactive Peptide B (SCP ), a neurallyBactive peptide, stimulates adenylate cyclaseactivity in parti

34、culate fractions of both heartand gill tissues with EC s of 0.1 and 1.0 M,50respectively.SQ22536 is an effective adenylate cyclase (AC)inhibitor.Purity: 98.10%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.41%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 m

35、g, 25 mg, 50 mg, 100 mg, 200 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/ST034307.html ST034307 HYPERLINK https:/www.MedChemE/ST034307.html HYPERLINK https:/www.MedChemE/tdi-10229.html TDI-10229Cat. No.: HY-101279 Cat. No.: HY-132298ST034307 is a potent and selective adenylyl cyclase1 (AC1) inhibitor, with IC of 2.3 M.50TDI-10229 is a potent and orally bioavailableinhibitor of soluble adenylyl cyclase (sAC,ADCY10)