Thrombin is a serine protease that in humans is encoded by the F2 gene. Thrombin is an intriguing coagulation protease demonstrating an array of effects on endothelial cells, vascular smooth muscle cells (VSMC), monocytes, and platelets, all of which are involved in the pathophysiology of atherosclerosis. There is mounting evidence that thrombin acts as a powerful modulator of many processes like regulation of vascular tone, permeability, migration and proliferation of VSMC, recruitment of monocytes into the atherosclerotic lesions, induction of diverse pro-inflammatory markers, and all of these are related to the progression of cardiovascular disease. Recent studies in transgenic mice models indicate that the deletion of the natural thrombin inhibitor heparin cofactor II promotes an accelerated atherogenic state. The combined evidence points to thrombin as a pivotal contributor to vascular pathophysiology.


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LX1606

Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

  • CAS Number: 1137608-69-5
  • MF: C36H35ClF3N7O6
  • MW: 754.155
  • Catalog: Tryptophan Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 145 °C
  • Flash Point: N/A

4-Ethynyl-L-phenylalanine

4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin[1].

  • CAS Number: 278605-15-5
  • MF: C11H11NO2
  • MW: 189.210
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 343.2±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 161.4±26.5 °C

DL-4-Chlorophenylalanine

Fenclonine is a pharmaceutical intermediate.

  • CAS Number: 7424-00-2
  • MF: C9H10ClNO2
  • MW: 199.634
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 339.5±32.0 °C at 760 mmHg
  • Melting Point: >240 °C (dec.)(lit.)
  • Flash Point: 159.1±25.1 °C

4-Ethynyl-L-phenylalanine hydrochloride

4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin[1].

  • CAS Number: 188640-63-3
  • MF: C11H12ClNO2
  • MW: 225.67
  • Catalog: Tryptophan Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fenclonine

4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2)[1].

  • CAS Number: 14173-39-8
  • MF: C9H10ClNO2
  • MW: 199.634
  • Catalog: 5-HT Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 339.5±32.0 °C at 760 mmHg
  • Melting Point: 235-238ºC
  • Flash Point: 159.1±25.1 °C

KAR-5585

Rodatristat ethyl (KAR5585) is an orally active tryptophan hydroxylase 1 (TPH1) inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH)[1][2].

  • CAS Number: 1673571-51-1
  • MF: C29H31ClF3N5O3
  • MW: 590.04
  • Catalog: Tryptophan Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KAR-5417

Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) inhibitor with an IC50 value of 33 nM, and shows robust reduction of intestinal serotonin (5-HT) levels in mice. Rodatristat also shows potent inhibition of TPH2 (IC50 of 7 nM)[1].

  • CAS Number: 1673568-73-4
  • MF: C27H27ClF3N5O3
  • MW: 561.98
  • Catalog: Tryptophan Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LP533401 HCI

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

  • CAS Number: 1040526-12-2
  • MF: C27H23ClF4N4O3
  • MW: 562.943
  • Catalog: Tryptophan Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Telotristat

Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

  • CAS Number: 1033805-22-9
  • MF: C27H26ClF3N6O3
  • MW: 574.982
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 704.7±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 380.0±35.7 °C

LX-1031

LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.

  • CAS Number: 945976-76-1
  • MF: C28H25F3N4O4
  • MW: 538.518
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 715.6±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 386.6±35.7 °C

Telotristat

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.

  • CAS Number: 1033805-28-5
  • MF: C25H22ClF3N6O3
  • MW: 546.92900
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.50±0.1 g/cm3 (20 ºC 760 Torr), 计算值
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PCPA methyl ester hydrochloride

PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability[1][2].

  • CAS Number: 14173-40-1
  • MF: C10H13Cl2NO2
  • MW: 250.122
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: 296.3ºC at 760 mmHg
  • Melting Point: 186-189 °C(lit.)
  • Flash Point: 133ºC

LP-533401

LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

  • CAS Number: 945976-43-2
  • MF: C27H22F4N4O3
  • MW: 526.482
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 699.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 376.5±34.3 °C

ACT-678689

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM[1].

  • CAS Number: 1783256-96-1
  • MF: C23H22ClFN6O4S2
  • MW: 565.040
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UNII:3I7LZ8M32B

6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes[1].

  • CAS Number: 7730-20-3
  • MF: C11H11FN2O2
  • MW: 222.216
  • Catalog: Tryptophan Hydroxylase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 450.7±45.0 °C at 760 mmHg
  • Melting Point: 280-285 °C (dec.)(lit.)
  • Flash Point: 226.4±28.7 °C