170809-51-5 Usage
Description
ASTRESSIN is a 30-membered homodetic cyclic peptide with the sequence D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-His-Lys-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2, cyclised by an amide bridge formed by condensation of the side-chain carboxy group of the Glu residue at position 19 and the side-chain amino group of the Lys residue at position 22.
Uses
Used in Neuroscience Research:
ASTRESSIN is used as a CRF-receptor antagonist for studying its effects on the decrease in the Schaffer collateral-CA1 field potential induced by hypoxia/hypoglycemia (ischemia) in rat hippocampal slices. This application helps researchers understand the role of CRF receptors in the brain's response to stress and ischemic conditions.
Biochem/physiol Actions
Astressin is a non-selective corticotropin releasing factor (CRF)-receptor antagonist. It potentially blocks CRF-induced adrenocorticotropic hormone (ACTH) release. Astressin effectively deceases delayed effects of chronic social isolation such as anxiety and fobial states in rats.
Enzyme inhibitor
This novel CRF antagonist (MW = 3663.20 g/mol; CAS 170809-51-5; Sequence: D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala- Glu-Gln-Ala-Gln-cyclo-(g-Glu-Ala-His-e-Lys)Asn-Arg-Leu-Leu-Mle-Glu- Ile-Ile-NH2; Solubility: 1 mg/mL in Acetic acid/water (10% vol/vol); Alternate Name: [D-Phe 12 , Nle 21,38 , Glu30 , Lys 33 ]-CRF) targets human Corticotropin-Releasing hormone (CRH) Receptor subtypes CRF2α (Ki = 1.5 nM) and CRF2β (Ki = 1 nM), with a comparable value (2 nM) for CRF1. (See also Antisauvagine-30; K41448) These type-2 GPCRs reside in plasma membranes of hormone-sensitive cells and bind CRH, a peptide hormone and neurotransmitter involved in stress responses. Astressin is a structurally constrained and competitive antagonists of corticotropin- releasing factor. Astressin is neuroprotective in the hippocampus when administered after a seizure. Peripheral injection of astressin blocks peripheral CRF- and abdominal surgery-induced delayed gastric emptying in rats. A related antagonist is Astressin 2B (FW = 4041.69 g/mol; CAS 681260-70-8; Sequence: Ac-Asp-Leu-Ser-D-Phe-His-a-methyl-Leu-Leu- Arg-Lys-Nle-Ile-Glu-Ile-Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala- cyclo-(g-Glu-Ala-Asn-e-Lys)Leu-Leu-Leu-Asp-a-methyl-Leu-Ile-NH2). Astressin 2B is a potent and selective antagonist of CRF2 (IC50 = 1.3 nM) and CRF1 (IC50 > 500 nM).
Check Digit Verification of cas no
The CAS Registry Mumber 170809-51-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,0,8,0 and 9 respectively; the second part has 2 digits, 5 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 170809-51:
(8*1)+(7*7)+(6*0)+(5*8)+(4*0)+(3*9)+(2*5)+(1*1)=135
135 % 10 = 5
So 170809-51-5 is a valid CAS Registry Number.
InChI:InChI=1/C161H269N49O42/c1-23-27-41-96(189-145(239)107(52-59-123(217)218)199-152(246)114(71-84(13)14)207-157(251)126(85(15)16)208-147(241)108(53-60-124(219)220)197-140(234)102(47-38-66-179-161(172)173)193-151(245)112(69-82(9)10)204-153(247)113(70-83(11)12)205-155(249)116(74-94-77-175-79-181-94)201-134(228)95(163)72-92-39-30-29-31-40-92)135(229)182-88(19)130(224)186-100(45-36-64-177-159(168)169)136(230)183-89(20)131(225)188-106(51-58-122(215)216)144(238)195-104(49-56-119(165)212)146(240)202-110(67-80(5)6)149(243)185-90(21)132(226)187-103(48-55-118(164)211)143(237)196-105-50-57-121(214)176-63-35-33-44-99(192-154(248)115(73-93-76-174-78-180-93)200-133(227)91(22)184-137(105)231)142(236)206-117(75-120(166)213)156(250)194-101(46-37-65-178-160(170)171)139(233)190-98(43-32-34-62-162)141(235)203-111(68-81(7)8)150(244)191-97(42-28-24-2)138(232)198-109(54-61-125(221)222)148(242)210-128(87(18)26-4)158(252)209-127(129(167)223)86(17)25-3/h29-31,39-40,76-91,95-117,126-128H,23-28,32-38,41-75,162-163H2,1-22H3,(H2,164,211)(H2,1
