Search Result

Results for "

TrkA inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) Adrenergic Receptor (4) Akt (1) Anaplastic lymphoma kinase (ALK) (9) Apoptosis (15) Autophagy (9) Bcr-Abl (1) c-Fms (2) c-Kit (4) c-Met/HGFR (6) Casein Kinase (1) CDK (2) Checkpoint Kinase (Chk) (1) Discoidin Domain Receptor (2) Drug Metabolite (1) E1/E2/E3 Enzyme (2) EGFR (2) FLT3 (7) Histamine Receptor (4) IGF-1R (1) Insulin Receptor (1) Isotope-Labeled Compounds (2) Itk (1) JAK (1) Ligands for Target Protein for PROTAC (1) mAChR (4) p62 (2) PDGFR (1) Pim (1) Polo-like Kinase (PLK) (1) RET (2) ROS Kinase (6) Serotonin Transporter (4) Sodium Channel (4) STAT (1) TAM Receptor (2) Tie (1) Trk Receptor (70) Tyrosinase (1) VEGFR (3)
By Research Areas:	Cancer (67) Cardiovascular Disease (1) Endocrinology (1) Infection (1) Inflammation/Immunology (8) Neurological Disease (17)

By Targets:

5-HT Receptor (4)

Adrenergic Receptor (4)

Akt (1)

Anaplastic lymphoma kinase (ALK) (9)

Apoptosis (15)

Autophagy (9)

Bcr-Abl (1)

c-Fms (2)

c-Kit (4)

c-Met/HGFR (6)

Casein Kinase (1)

CDK (2)

Checkpoint Kinase (Chk) (1)

Discoidin Domain Receptor (2)

Drug Metabolite (1)

E1/E2/E3 Enzyme (2)

EGFR (2)

FLT3 (7)

Histamine Receptor (4)

IGF-1R (1)

Insulin Receptor (1)

Isotope-Labeled Compounds (2)

Itk (1)

JAK (1)

Ligands for Target Protein for PROTAC (1)

mAChR (4)

p62 (2)

PDGFR (1)

Pim (1)

Polo-like Kinase (PLK) (1)

RET (2)

ROS Kinase (6)

Serotonin Transporter (4)

Sodium Channel (4)

STAT (1)

TAM Receptor (2)

Tie (1)

Trk Receptor (70)

Tyrosinase (1)

VEGFR (3)

By Research Areas:

Cancer (67)

Cardiovascular Disease (1)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (8)

Neurological Disease (17)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-151948

TrkA-IN-3	Trk Receptor	Neurological Disease
TrkA-IN-3 is a potent, subselective and allosteric *TrkA* inhibitor, with an IC₅₀ of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain .

HY-151949

TrkA-IN-4	Trk Receptor	Neurological Disease
TrkA-IN-4, a potent, orally active and allosteric *TrkA* inhibitor, is a proagent of TrkA-IN-3 (IC₅₀=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects .

HY-129634

TrkA-IN-1	Trk Receptor	Neurological Disease
TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC₅₀ of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity .

HY-157168

TrkA-IN-6	Trk Receptor	Neurological Disease
TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC₅₀ of 68.99 μM .

HY-161775

RET/TRKA-IN-1	RET Trk Receptor	Cancer
RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC₅₀=0.375 µM) and *TRKA. RET/TRKA-IN-1 inhibits* cell viability of LC-2 and KM12, with GI₅₀ of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase .

HY-161819

TRK-IN-29	Trk Receptor	Cancer
TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC₅₀: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA ^G595R, TRKA ^F589L, TRKA ^G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .

HY-144069

Pan-Trk-IN-3	Trk Receptor Apoptosis	Cancer
Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC₅₀ values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against *TrkA, TrkB, TrkC, TrkA* ^G595R, TrkA ^G667C, TrkA ^G667S, TrkA ^F589L and TrkC ^G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .

HY-163004

Type II TRK inhibitor 2	Trk Receptor	Cancer
Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA ^G595R and Ba/F3-TRKA ^G667C cell proliferation (IC₅₀: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .

HY-146749

FLT3/TrKA-IN-1	FLT3 Trk Receptor Apoptosis	Cancer
FLT3/TrKA-IN-1 is a potent *FLT3/TrKA* dual kinase inhibitor with the IC₅₀s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .

HY-157542

CG428-NEG	Others	Others
CG428-NEG is a TRK degrader negative control. CG428-NEG inhibits cell growth and reduce TPM3-TRKA levels .

HY-141864

ITK/TRKA-IN-1	Itk	Inflammation/Immunology
ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC₅₀ value of 1.0 nM and 96 % inhibition, respectively.

HY-164514

NMS-P626	Trk Receptor	Cancer
NMS-P626 is an inhibitor of *TRKA, TRKB, and TRKC, with IC₅₀* values of 8 nM, 7 nM, and 3 nM, respectively. NMS-P626 inhibits the growth of KM12 cells by suppressing the phosphorylation of *TPM3-TRKA* and downstream signaling in KM12 cells, with an IC₅₀ of 19 nM for KM12 cells. NMS-P626 can be used in colorectal cancer research .

HY-164517

ONO-7579	Trk Receptor	Cancer
ONO-7579 is an orally active *TRKA* inhibitor that suppresses tumor growth by inhibiting the phosphorylation of *TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA* in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research .

HY-149965

TRK-IN-23	Trk Receptor Apoptosis	Cancer
TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC₅₀ values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against *TRKA, TRKC, TRKA* ^G595R, TRKA ^F589L, and TRKA ^G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells .

HY-146755

TIY-7	Trk Receptor	Cancer
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC₅₀s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA ^G595R, TRKA ^G667C, TRKA ^F589L, TRKC ^G623R, TRKC ^G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .

HY-146115

TRK-IN-19	Trk Receptor	Cancer
TRK-IN-19 (Compound I-10 ) is a potent inhibitor of TRK (TRKA IC₅₀ = 1.1 nM, TRKA ^G595R IC₅₀ = 5.3 nM). TRK-IN-19 has the potential for the research of cancer diseases .

HY-132229

LPM4870108	Trk Receptor	Cancer
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC₅₀s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, *TrkA, TrkA* ^G595R and TrkA ^G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC₅₀=182 nM). LPM4870108 exhibits anti-tumor activity .

HY-144690

D5261	Trk Receptor	Cancer
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor .

HY-156086

TRK-IN-24	Trk Receptor	Cancer
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA ^G595R, TRKA ^G667C and TRKA ^F589L IC₅₀s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 ^G595R and BaF3-CD74-NTRK1 ^G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC₅₀ of 1.43-47.56 nM .

HY-153745

Protein kinase inhibitor 5	Trk Receptor	Cancer
Protein kinase inhibitor 5 is a potent *TRK-A* inhibitor with an IC₅₀ value of 1.8 nM. Protein kinase inhibitor 5 inhibits cell viability .

HY-153745A

Protein kinase inhibitor 5 sulfate hydrate	Trk Receptor	Cancer
Protein kinase inhibitor 5 sulfate hydrate is a potent *TRK-A* inhibitor with an IC₅₀ value of 1.8 nM. Protein kinase inhibitor 5 sulfate hydrate inhibits cell viability .

HY-137465

CG428	Trk Receptor	Cancer
CG428 is a potent and selective tropomyosin receptor kinase (TRK) degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC₅₀ = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC₅₀ = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (K_d = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC₅₀ = 2.9 nM) .

HY-153743

Protein kinase inhibitor 4	ROS Kinase Trk Receptor	Cancer
Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits *TRK-A* and ROS1 (IC₅₀=3.0 nM and 104 nM respectively) .

HY-17603

Belizatinib 1 Publications Verification TSR-011	Anaplastic lymphoma kinase (ALK) Trk Receptor	Cancer
Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC₅₀ of 0.7 nM for wild-type recombinant ALK kinase.

HY-144424

Trk-IN-11	Trk Receptor	Cancer
Trk-IN-11 (Compound 14h) is a potent inhibitor of TRK (IC₅₀ = 1.4, 1.8 nM, against TrkA, TrkA ^G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-11 has the potential for the research of cancer disease .

HY-50867

Lestaurtinib 3 Publications Verification CEP-701; KT-5555	JAK FLT3 Trk Receptor Apoptosis STAT	Cancer
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the *TrkA/B/C* domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC₅₀s of 2, 25 and 0.9 nM for FLT3, *TrkA* and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .

HY-112423

CE-245677	Trk Receptor Tie	Cardiovascular Disease Cancer
CE-245677 is a potent reversible inhibitor of Tie2 and *TrkA/B* kinases with a cellular IC₅₀s of 4.7 and 1 nM.

HY-131244

ALK-IN-9	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC₅₀s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .

HY-150258

TRK-IN-22	Trk Receptor	Others
TRK-IN-22 (compound 11) is a TRK inhibitor. TRK-IN-22 (compound 11), a typical type I inhibitor, covers the ATP-binding pocket of TRKA .

HY-101977

Selitrectinib 4 Publications Verification LOXO-195	Trk Receptor	Cancer
Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for *TRKA* and TRKC, respectively .

HY-164483

HS-345	Akt Trk Receptor	Cancer
HS-345 is a *TrkA/Ak* inhibitor with significant anti-pancreatic cancer effects. HS-345 inhibits the growth and proliferation of pancreatic cancer cells by targeting the *TrkA/Akt* signaling pathway, while also inducing apoptosis. Additionally, HS-345 suppresses blood vessel formation by decreasing the expression of HIF-1α and VEGF. HS-345 holds promise for research in pancreatic cancer .

HY-12866B

(R)-Larotrectinib (R)-LOXO-101; (R)-ARRY-470	Trk Receptor	Infection Inflammation/Immunology Cancer
(R)-Larotrectinib is a potent TRK inhibitor with an IC₅₀ value of 28.5 nM for TrkA. (R)-Larotrectinib can be used for researching cancer, inflammatory and certain infectious diseases

HY-145587

Paltimatrectinib PBI-200; PPI-5278	Tyrosinase Trk Receptor	Inflammation/Immunology Cancer
Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC₅₀ of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases .

HY-12327

Trk-IN-1	Trk Receptor	Neurological Disease Cancer
Trk-IN-1 (example 9), a potent tropomyosin-related kinase (Trk) inhibitor, shows potency against TrkA (3.7 nM) and TrkB (94 nM), respectively .

HY-144423

Trk-IN-10	Trk Receptor	Cancer
Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC₅₀ = 0.86, 6.92 nM, against TrkA, TrkA ^G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-10 (IC₅₀ = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity .

HY-151945

TRK II-IN-1	Trk Receptor FLT3 VEGFR RET	Cancer
TRK II-IN-1 is a potent type II TRK inhibitor, with IC₅₀s of 3.3, 6.4, 4.3 and 9.4 nM, for *TRKA/B/C* and TRKA ^G667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC₅₀s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers .

HY-118271

GNF-8625	Ligands for Target Protein for PROTAC Trk Receptor	Cancer
GNF-8625 is a broad-spectrum TRK inhibitor that can combine with Thalidomide to form a PROTAC degrader. The IC50 of GNF-8625 for inhibiting TRKA, TRKB, and TRKC are 0.8 nM, 22 nM, and 5.4 nM, respectively.

HY-126287

JND4135	Trk Receptor Apoptosis	Cancer
JND4135 is a Type II TRK inhibitor with IC₅₀ values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .

HY-163366

TRK-IN-28	Trk Receptor	Cancer
TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC₅₀ values of 0.55 nM, 25.1 nM and 5.4 nM against TRK ^WT, TRK ^G595R and TRK ^G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC₅₀ values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA ^WT, Ba/F3-ETV6-TRKB ^WT, Ba/F3-LMNA-TRK ^G595R and Ba/F3-LMNA-TRKA ^G667C, respectively .

HY-18314

GW 441756 5+ Cited Publications	Trk Receptor Apoptosis	Neurological Disease Cancer
GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC₅₀=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth .

HY-12866

Larotrectinib 5+ Cited Publications LOXO-101; ARRY-470	Trk Receptor Apoptosis	Cancer
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

HY-112437

PF-06737007	Trk Receptor	Neurological Disease
PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 7.7 nM, 15 nM and 3.9 nM for *TrkA, TrkB* and TrkC, respectively . Anti-hyperalgesic effect .

HY-112434

PF-06733804	Trk Receptor	Neurological Disease
PF-06733804 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 8.4 nM, 6.2 nM and 2.2 nM for *TrkA, TrkB* and TrkC, respectively . Anti-hyperalgesic effect .

HY-146807

Type II TRK inhibitor 1	Trk Receptor	Cancer
Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA ^G667C and ETV6-TRKC ^G696C fusion proteins with IC₅₀s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-101977R

Selitrectinib (Standard)	Trk Receptor	Cancer
Selitrectinib (Standard) is the analytical standard of Selitrectinib. This product is intended for research and analytical applications. Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for *TRKA* and TRKC, respectively .

HY-136535

Anizatrectinib hTrkA-IN-1	Trk Receptor	Inflammation/Immunology
Anizatrectinib (hTrkA-IN-1) is a potent and orally active inhibitor of TrkA kinase with an IC₅₀ of 1.3 nM, compound 2 extracted from patent WO2015175788. Anizatrectinib can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al .

HY-112436

PF-6683324 Trk-IN-4	Trk Receptor	Neurological Disease
PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 1.9 nM, 2.6 nM and 1.1 nM for *TrkA, TrkB* and TrkC, respectively . Anti-hyperalgesic effect .

HY-101977B

(3aR)-Selitrectinib (3aR)-LOXO-195	Trk Receptor	Cancer
(3aR)-Selitrectinib ((3aR)-LOXO-195) is an isform of Selitrectinib (HY-101977), which is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for *TRKA* and TRKC, respectively .

HY-12866A

Larotrectinib sulfate 5+ Cited Publications LOXO-101 sulfate; ARRY-470 sulfate	Trk Receptor Apoptosis	Cancer
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

HY-15590

AZ-23 3 Publications Verification AZ23; AZ 23	Trk Receptor	Cancer
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC₅₀s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.

Cat. No.	Product Name	Target	Research Area

HY-P3709A

TRAF6 peptide TFA	p62 E1/E2/E3 Enzyme	Neurological Disease
TRAF6 peptide TFA is a specific TRAF6-p62 inhibitor. TRAF6 peptide TFA potently abrogates NGF-dependent *TrkA* ubiquitination. TRAF6 peptide TFA has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke .

HY-P3709

TRAF6 peptide	p62 E1/E2/E3 Enzyme	Neurological Disease
TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent *TrkA* ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke .

Cat. No.	Product Name	Target	Research Area

HY-P99297

Bedinvetmab ZTS-00508841	Trk Receptor	Inflammation/Immunology
Bedinvetmab (ZTS-00508841) is a canine monoclonal antibody (mAb) targeting nerve growth factor (NGF). Bedinvetmab inhibits NGF interaction with tropomyosin receptor kinase A (trkA) and p75 neurotrophin receptor (p75NTR) receptors. Bedinvetmab can be used for the research of osteoarthritis pain in dogs .

Cat. No.	Product Name	Chemical Structure

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].

HY-12678S1

Entrectinib-d8

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .

HY-12678S

Entrectinib-d4

Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC₅₀ values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .

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