PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II
2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
CAS: 729589-58-6
Molecular Formula: C36H63N11O8
PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II - Names and Identifiers
PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II - Physico-chemical Properties
| Molecular Formula | C36H63N11O8 |
| Molar Mass | 777.95 |
| Appearance | powder |
| Color | white |
| Storage Condition | -20°C |
| In vitro study | 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH 2 ) is equally effective to and 10 to 25 times more potent than SLIGRLNH 2 for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively. In bioassays of tissue PAR2 activity, measured as arterial vasodilation and hyperpolarization, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH 2 ) is 10 to 300 times more potent than SLIGRL-NH 2 . Unlike trans-cinnamoyl-LIGRLO-NH 2 , 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries. |
| In vivo study | Furoyl-LIGRLO-amide (injected intradermally at the nape of the neck; 10 μg; pre-injected) exhibits fewer scratches in response to 2-Furoyl-LIGRLO-amide but not to histamine in Trpv3 -/- mice. But it decreases significantly the number of scratches in WT mice. Animal Model: Adult male (2/3-month-old) Trpv3 -/- and WT mice Dosage: 10 μg Administration: Injected intradermally at the nape of the neck Result: Was involved in PAR2- induced acute itch. |
PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II - Reference Information
| biological activity | 2-Furoyl-LIGRLO-amide is a potent selective protease-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0. |
| target | Proteinase-activated receptor 2 (PAR2) |
| in vitro study | 2-furoyl-ligro-amide (2-furoyl-ligro-nh2) is equally effective to and 10 to 25 times more potent than SLIGRLNH 2 for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively. In bioassays of tissp2 activity, measured as arterial vasodilation and hyperpolarization, 2-furoyl-ligro-amide (2-furoyl-ligro-nh2) is 10 to 300 times more than SLIGRL-NH 2 . Unlike trans-cinnamoyl-LIGRLO-NH 2, 2-furoyl-ligrlo-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries. |
| in vivo research | Furoyl-LIGRLO-amide (injected intradermally at the neck of the neck; 10 μg; pre-injected) exhibits fewer scratches in response to 2-furoyl-ligrlo-amide but not to histamine in trpv3-/- mice. but it decreases significantly the number of scratches in wtmice. animal model: adult male (2/3-month-old) trpv3-/- and wtmice dosage: 10 μ g Administration: Injected intradermally at the nape of the neck result: was involved in PAR2- induced acute itch. |
| Animal Model: | Adult male (2/3-month-old) Trpv3 -/- and WT mice |
| Dosage: | 10 μg |
| Administration: | Injected intradermally at the nape of the neck |
| Result: | Was involved in PAR2- induced acute itch. |
Last Update：2024-04-09 21:04:16
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View History
PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II
(3-氨基-4-吡啶基)甲醇
(4-哌啶基)乙酸甲酯盐酸盐
4-溴-2-三甲基硅烷基噻唑
[3-(哌啶-1-基甲基)苯基]胺
4-乙酰苯基三氟甲烷磺酸酯
2-(吡咯啉基磺酰基)苯硼酸
1 2 3 4-TETRAHYDROCYCLOPENT(B) INDOLE
2-(嘧啶-4-基)乙酸乙酯
6-溴苯并[D]噻唑-2-甲酰胺
(3-氨基-4-吡啶基)甲醇
(4-哌啶基)乙酸甲酯盐酸盐
4-溴-2-三甲基硅烷基噻唑
[3-(哌啶-1-基甲基)苯基]胺
4-乙酰苯基三氟甲烷磺酸酯
2-(吡咯啉基磺酰基)苯硼酸
1 2 3 4-TETRAHYDROCYCLOPENT(B) INDOLE
2-(嘧啶-4-基)乙酸乙酯
6-溴苯并[D]噻唑-2-甲酰胺