K 41498Highly selective and potent CRF2 antagonist CAS# 434938-41-7 |
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Quality Control & MSDS
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| Cas No. | 434938-41-7 | SDF | Download SDF |
| PubChem ID | 90488734 | Appearance | Powder |
| Formula | C162H276N48O46 | M.Wt | 3632.26 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 5 mg/ml in water | ||
| Sequence | FHLLRKXIEIEKQEKEKQQAANNRLLLDTI (Modifications: Phe-1 = D-Phe, X = Nle, Ile-30 = C-terminal amide) | ||
| SMILES | CCCCC(C(=O)NC(C(C)CC)C(=O)NC(CCC(=O)O)C(=O)NC(C(C)CC)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(C)C(=O)NC(C)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)O)C(=O)NC(C(C)O)C(=O)NC(C(C)CC)C(=O)N)NC(=O)C(CCCCN)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC=N1)NC(=O)C(CC2=CC=CC=C2)N | ||
| Standard InChIKey | QJWWADQIQXXJQA-DCUOZLBZSA-N | ||
| Standard InChI | InChI=1S/C162H276N48O46/c1-21-25-41-94(184-136(232)95(42-29-33-62-163)185-140(236)99(46-37-66-179-161(174)175)189-149(245)108(68-80(5)6)201-152(248)111(71-83(11)12)204-154(250)113(74-92-78-178-79-181-92)199-134(230)93(167)73-91-39-27-26-28-40-91)147(243)208-128(86(16)23-3)159(255)197-107(54-61-125(223)224)148(244)209-129(87(17)24-4)158(254)196-106(53-60-124(221)222)146(242)188-97(44-31-35-64-165)138(234)193-103(50-57-119(170)214)143(239)195-105(52-59-123(219)220)145(241)187-98(45-32-36-65-166)139(235)194-104(51-58-122(217)218)144(240)186-96(43-30-34-63-164)137(233)192-102(49-56-118(169)213)142(238)191-101(48-55-117(168)212)135(231)183-88(18)132(228)182-89(19)133(229)198-114(75-120(171)215)156(252)205-115(76-121(172)216)155(251)190-100(47-38-67-180-162(176)177)141(237)200-109(69-81(7)8)150(246)202-110(70-82(9)10)151(247)203-112(72-84(13)14)153(249)206-116(77-126(225)226)157(253)210-130(90(20)211)160(256)207-127(131(173)227)85(15)22-2/h26-28,39-40,78-90,93-116,127-130,211H,21-25,29-38,41-77,163-167H2,1-20H3,(H2,168,212)(H2,169,213)(H2,170,214)(H2,171,215)(H2,172,216)(H2,173,227)(H,178,181)(H,182,228)(H,183,231)(H,184,232)(H,185,236)(H,186,240)(H,187,241)(H,188,242)(H,189,245)(H,190,251)(H,191,238)(H,192,233)(H,193,234)(H,194,235)(H,195,239)(H,196,254)(H,197,255)(H,198,229)(H,199,230)(H,200,237)(H,201,248)(H,202,246)(H,203,247)(H,204,250)(H,205,252)(H,206,249)(H,207,256)(H,208,243)(H,209,244)(H,210,253)(H,217,218)(H,219,220)(H,221,222)(H,223,224)(H,225,226)(H4,174,175,179)(H4,176,177,180)/t85-,86-,87-,88-,89-,90+,93+,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,127-,128-,129-,130-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and highly selective CRF2 receptor antagonist (Ki values are 0.66, 0.62 and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. In rats in vivo, blocks urocortin-induced hypotension following systemic administration. |
K 41498 Dilution Calculator
K 41498 Molarity Calculator
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The highly selective CRF(2) receptor antagonist K41498 binds to presynaptic CRF(2) receptors in rat brain.[Pubmed:12110614]
Br J Pharmacol. 2002 Jul;136(6):896-904.
1. Novel analogues of antisauvagine-30 (aSvg-30), a selective antagonist for CRF(2) receptors, have been synthesized and characterized in vitro and in vivo. 2. The analogues were tested for their ability to compete for [(125)I-Tyr(0)]Svg binding and to inhibit Svg-stimulated adenylate cyclase activity in human embryonic kidney (HEK) 293 cells, permanently transfected with cDNA coding for the human CRF(1) (hCRF(1)), hCRF(2alpha) and hCRF(2beta) receptor. One analogue [D-Phe(11), His(12), Nle(17)]Svg(11-40), named K41498, showed high affinity binding to hCRF(2alpha) (K(i)=0.66+/-0.03 nM) and hCRF(2beta) (K(i)=0.62+/-0.01 nM) but not the hCRF(1) receptor (k(i)=425+50 nM) and decreased Svg-stimulated cAMP accumulation in hCRF(2) expressing cells. In conscious Wistar-Kyoto rats, K41498 (1.84 microg, i.v.) antagonized the hypotensive response to systemic urocortin (1.4 microg, i.v.), but did not block the pressor response to centrally administered urocortin (2.35 microg, i.c.v.). 3. K41498 was subsequently radio-iodinated, and in autoradiographic studies, specific (sensitive to rat urocortin, astressin and aSvg30, but insensitive to antalarmin) binding of (125)I-K41498 (100 pM) was detected in the heart and in selected brain regions including the nucleus tractus solitarius (NTS), spinal trigeminal nucleus, lateral septum and around the anterior and middle cerebral arteries. 4. Following unilateral nodose ganglionectomy, binding of (125)I-K41498 was reduced by 65% in the ipsilateral NTS, indicative of presynaptic CRF(2) receptors on vagal afferent terminals. 5. These data demonstrate that K41498 is a useful tool to study native CRF(2) receptors in the brain and periphery.
Design, synthesis and pharmacological characterization of new highly selective CRF(2) antagonists: development of 123I-K31440 as a potential SPECT ligand.[Pubmed:11835994]
Peptides. 2002 Mar;23(3):453-60.
Novel analogs of antisauvagine-30 (aSvg-30), a specific antagonist for corticotropin-releasing factor (CRF) receptor, type 2 (CRF(2)), have been synthesized and characterized in vitro and in vivo. The N-terminal amino acid D-phenylalanine in aSvg-30 was replaced by a D-tyrosine residue for specific radioactive labeling with 123I. Additionally, Met(17) of aSvg-30 was substituted by norleucine and the N-terminus of the peptide was acetylated to increase in vivo metabolic stability. The aSvg-30 analogs were tested for their ability to displace [125I-Tyr(0)]Svg in binding experiments and to inhibit Svg-stimulated adenylate cyclase activity in human embryonic kidney (HEK) 293 cells, permanently transfected with cDNA coding for the human CRF(1) (hCRF(1)), hCRF(2alpha) and hCRF(2beta) receptor. Ac-[D-Tyr(11), His(12), Nle(17)Svg(11-40), named K31440, showed high specific binding to hCRF(2alpha) (K(i) = 1.48 +/- 0.34 nM) and hCRF(2beta) (K(i) = 2.05 +/- 0.61 nM) but not the hCRF(1) receptor (K(i) = 288 +/- 13 nM) and decreased Svg-stimulated cAMP activity in hCRF(2)-expressing cells in a similar fashion as aSvg-30. In biodistribution studies specific uptake of 123I-K31440 was detected after 1 h in small intestine of BALB/c nude mice. These data demonstrate that 123I-K31440 may serve as a useful tool to detect native CRF(2) receptors and elucidate their role in gastrointestinal disorders and diseases such as irritable bowel syndrome or cancer.
