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189388-22-5

中文名稱 TYR-PRO-TRP-PHE-NH2
英文名稱 ENDOMORPHIN-1
CAS 189388-22-5
分子式 C34H38N6O5
MDL 編號(hào) MFCD01321063
分子量 610.7
MOL 文件 189388-22-5.mol
更新日期 2024/12/23 10:30:25
189388-22-5 結(jié)構(gòu)式 189388-22-5 結(jié)構(gòu)式

基本信息

中文別名
內(nèi)嗎啡 1
內(nèi)嗎啡肽 1
英文別名
ENDOMORPHIN-1

物理化學(xué)性質(zhì)

熔點(diǎn)144-146℃
沸點(diǎn)1052.8±65.0 °C(Predicted)
密度1.343±0.06 g/cm3(Predicted)
RTECS號(hào)SQ7316800
儲(chǔ)存條件−20°C
儲(chǔ)存條件−20°C
溶解度≥14.9 mg/mL in H2O; ≥30.55 mg/mL in DMSO; ≥47 mg/mL in EtOH
酸度系數(shù)(pKa)9.86±0.15(Predicted)
形態(tài)固體
顏色白色至灰白色
水溶解性溶于水
CAS 數(shù)據(jù)庫189388-22-5(CAS DataBase Reference)

安全數(shù)據(jù)

WGK Germany3
WGK Germany3

知名試劑公司產(chǎn)品信息

TYR-PRO-TRP-PHE-NH2價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-P0185TYR-PRO-TRP-PHE-NH2
Endomorphin 1
189388-22-55mg500元
2024/11/08HY-P0185TYR-PRO-TRP-PHE-NH2
Endomorphin 1
189388-22-510mM * 1mLin Water672元
2024/11/08HY-P0185TYR-PRO-TRP-PHE-NH2
Endomorphin 1
189388-22-510mg700元

常見問題列表

生物活性
Endomorphin 1,一種高度選擇性的高親和力μ-opioid受體激動(dòng)劑 , 對(duì)kappa3結(jié)合位點(diǎn)具有高親和力 ,Ki為 20 到 30 nM 之間。
靶點(diǎn)

Ki: 20-30 nM (kappa 3 opioid receptor)

體外研究

Endomorphin 1 (EM-1) is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 2 (EM-2). The two Endomorphins display reasonable affinities for kappa 3 binding sites, with K i values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ 1 and μ 2 receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa 1 binding sites, with K i values greater than 500 nM.

體內(nèi)研究

Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice.

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