K 41498Highly selective and potent CRF2 antagonist CAS# 434938-41-7 |
- CX-4945 (Silmitasertib)
Catalog No.:BCC3693
CAS No.:1009820-21-6
- GF 109203X
Catalog No.:BCC3704
CAS No.:133052-90-1
- Go 6983
Catalog No.:BCC3705
CAS No.:133053-19-7
- Go 6976
Catalog No.:BCC3703
CAS No.:136194-77-9
- Enzastaurin (LY317615)
Catalog No.:BCC1100
CAS No.:170364-57-5
- Staurosporine
Catalog No.:BCC3612
CAS No.:62996-74-1
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
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. |
||
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. |
||
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
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- Dacarbazine
Catalog No.:BCC1174
CAS No.:4342-03-4
- Nandrolone
Catalog No.:BCC9086
CAS No.:434-22-0
- Lithocholic Acid
Catalog No.:BCC3805
CAS No.:434-13-9
- Oxymetholone
Catalog No.:BCC4692
CAS No.:434-07-1
- Methenolone acetate
Catalog No.:BCC9028
CAS No.:434-05-9
- Ethisterone
Catalog No.:BCC4478
CAS No.:434-03-7
- VU 0357121
Catalog No.:BCC4595
CAS No.:433967-28-3
- 3-O-Acetyloleanolic acid
Catalog No.:BCN5486
CAS No.:4339-72-4
- Toddaculine
Catalog No.:BCN3639
CAS No.:4335-12-0
- Boc-Tyr-OMe
Catalog No.:BCC3459
CAS No.:4326-36-7
- 6-Hydroxykaempferol
Catalog No.:BCN3334
CAS No.:4324-55-4
- Formoterol Hemifumarate
Catalog No.:BCC4349
CAS No.:43229-80-7
- L-5-Hydroxytryptophan
Catalog No.:BCC8106
CAS No.:4350-09-8
- H-Arg(Tos)-OH
Catalog No.:BCC2867
CAS No.:4353-32-6
- 5-Hydroxy-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[5,6-f][1,3]benzodioxol-8-one
Catalog No.:BCC8350
CAS No.:4354-76-1
- (-)-Curine
Catalog No.:BCN2673
CAS No.:436-05-5
- Diffractic Acid
Catalog No.:BCN8506
CAS No.:436-32-8
- Fangchinoline
Catalog No.:BCN5956
CAS No.:436-77-1
- Ajmaline
Catalog No.:BCN3867
CAS No.:4360-12-7
- JKC 363
Catalog No.:BCC6022
CAS No.:436083-30-6
- Kobe0065
Catalog No.:BCC5290
CAS No.:436133-68-5
- Tetrodotoxin
Catalog No.:BCN1035
CAS No.:4368-28-9
- MRS 2365
Catalog No.:BCC5879
CAS No.:436847-09-5
- Gentisin
Catalog No.:BCN7518
CAS No.:437-50-3
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.